pyridines

Summary

Summary: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

Top Publications

  1. doi Sorafenib in advanced hepatocellular carcinoma
    Josep M Llovet
    Barcelona Clinic Liver Cancer Group, Institut d Investigacions Biomediques August Pi i Sunyer, Centro de Investigaciones en Red de Enfermedades Hepáticas y Digestivas Hospital Clínic Barcelona, Barcelona
    N Engl J Med 359:378-90. 2008
  2. doi Dabigatran versus warfarin in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 361:1139-51. 2009
  3. doi Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial
    Ann Lii Cheng
    National Taiwan University Hospital, Taipei, Taiwan
    Lancet Oncol 10:25-34. 2009
  4. ncbi BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis
    Scott M Wilhelm
    Bayer Pharmaceuticals Corporation, West Haven, Connecticut 06516, USA
    Cancer Res 64:7099-109. 2004
  5. doi Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling
    Scott M Wilhelm
    Bayer HealthCare Pharmaceuticals, 340 Changebridge Road, P O Box 1000, Montville, NJ 07045 1000, USA
    Mol Cancer Ther 7:3129-40. 2008
  6. doi Dabigatran etexilate--a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity
    Joanne van Ryn
    Department of Drug Discovery Support, Boehringer Ingelheim Pharma GmbH and Co KG, Biberach an der Riss, Germany
    Thromb Haemost 103:1116-27. 2010
  7. doi Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma
    Robert L Yauch
    Genentech, South San Francisco, CA 94080, USA
    Science 326:572-4. 2009
  8. pmc Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)
    Linda Vermeulen
    Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
    EMBO J 22:1313-24. 2003
  9. doi Inhibition of the hedgehog pathway in advanced basal-cell carcinoma
    Daniel D Von Hoff
    Translational Genomics Research Institute and Scottsdale Healthcare, Scottsdale, AZ, USA
    N Engl J Med 361:1164-72. 2009
  10. doi Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449
    Charles M Rudin
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
    N Engl J Med 361:1173-8. 2009

Detail Information

Publications350 found, 100 shown here

  1. doi Sorafenib in advanced hepatocellular carcinoma
    Josep M Llovet
    Barcelona Clinic Liver Cancer Group, Institut d Investigacions Biomediques August Pi i Sunyer, Centro de Investigaciones en Red de Enfermedades Hepáticas y Digestivas Hospital Clínic Barcelona, Barcelona
    N Engl J Med 359:378-90. 2008
    ..A preliminary study suggested that sorafenib, an oral multikinase inhibitor of the vascular endothelial growth factor receptor, the platelet-derived growth factor receptor, and Raf may be effective in hepatocellular carcinoma...
  2. doi Dabigatran versus warfarin in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 361:1139-51. 2009
    ..Warfarin reduces the risk of stroke in patients with atrial fibrillation but increases the risk of hemorrhage and is difficult to use. Dabigatran is a new oral direct thrombin inhibitor...
  3. doi Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial
    Ann Lii Cheng
    National Taiwan University Hospital, Taipei, Taiwan
    Lancet Oncol 10:25-34. 2009
    ....
  4. ncbi BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis
    Scott M Wilhelm
    Bayer Pharmaceuticals Corporation, West Haven, Connecticut 06516, USA
    Cancer Res 64:7099-109. 2004
    ..These data demonstrate that BAY 43-9006 is a novel dual action RAF kinase and VEGFR inhibitor that targets tumor cell proliferation and tumor angiogenesis...
  5. doi Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling
    Scott M Wilhelm
    Bayer HealthCare Pharmaceuticals, 340 Changebridge Road, P O Box 1000, Montville, NJ 07045 1000, USA
    Mol Cancer Ther 7:3129-40. 2008
    ..In particular, preclinical evidence that supports the different mechanisms of action of sorafenib is discussed...
  6. doi Dabigatran etexilate--a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity
    Joanne van Ryn
    Department of Drug Discovery Support, Boehringer Ingelheim Pharma GmbH and Co KG, Biberach an der Riss, Germany
    Thromb Haemost 103:1116-27. 2010
    ....
  7. doi Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma
    Robert L Yauch
    Genentech, South San Francisco, CA 94080, USA
    Science 326:572-4. 2009
    ..These findings show that acquired mutations in a serpentine receptor with features of a G protein-coupled receptor can serve as a mechanism of drug resistance in human cancer...
  8. pmc Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)
    Linda Vermeulen
    Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
    EMBO J 22:1313-24. 2003
    ..This effect represents, together with phosphorylation of nucleosome components such as histone H3, an essential step leading to selective transcriptional activation of NF-kappaB-dependent gene expression...
  9. doi Inhibition of the hedgehog pathway in advanced basal-cell carcinoma
    Daniel D Von Hoff
    Translational Genomics Research Institute and Scottsdale Healthcare, Scottsdale, AZ, USA
    N Engl J Med 361:1164-72. 2009
    ..In a phase 1 clinical trial, we assessed the safety and pharmacokinetics of GDC-0449, a small-molecule inhibitor of SMO, and responses of metastatic or locally advanced basal-cell carcinoma to the drug...
  10. doi Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449
    Charles M Rudin
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
    N Engl J Med 361:1173-8. 2009
    ....
  11. pmc Phase II trial of sorafenib in advanced thyroid cancer
    Vandana Gupta-Abramson
    Developmental TherapeuticsProgram of the Abramson CancerCenter, University of Pennsylvania, Philadelphia, PA 19104, USA
    J Clin Oncol 26:4714-9. 2008
    ....
  12. pmc Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis
    T Eisen
    Royal Marsden Hospital, Downs Road, Surrey SMT 5PT, UK
    Br J Cancer 95:581-6. 2006
    ..i.d.). Ongoing trials in advanced melanoma are evaluating sorafenib combination therapies...
  13. ncbi Sorafenib in advanced clear-cell renal-cell carcinoma
    Bernard Escudier
    Department of Medicine, Institut Gustave Roussy, Villejuif, France
    N Engl J Med 356:125-34. 2007
    ..We conducted a phase 3, randomized, double-blind, placebo-controlled trial of sorafenib, a multikinase inhibitor of tumor-cell proliferation and angiogenesis, in patients with advanced clear-cell renal-cell carcinoma...
  14. doi Efficacy and safety of dabigatran compared with warfarin at different levels of international normalised ratio control for stroke prevention in atrial fibrillation: an analysis of the RE-LY trial
    Lars Wallentin
    Uppsala Clinical Research Centre, Uppsala University, Uppsala, Sweden
    Lancet 376:975-83. 2010
    ..We aimed to investigate the primary and secondary outcomes of the RE-LY trial in relation to each centre's mean TTR (cTTR) in the warfarin population...
  15. ncbi Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo
    David B Ring
    Chiron Corporation, Emeryville, California, USA
    Diabetes 52:588-95. 2003
    ..Collectively, our results suggest that these selective GSK-3 inhibitors may be useful as acute-acting therapeutics for the treatment of the insulin resistance of type 2 diabetes...
  16. ncbi Activation of p38 mitogen-activated protein kinase in spinal microglia is a critical link in inflammation-induced spinal pain processing
    Camilla I Svensson
    Department of Anesthesiology, University of California, San Diego, La Jolla, California, USA
    J Neurochem 86:1534-44. 2003
    ..Taken together, these results indicate that spinal p38 MAPK is involved in inflammation-induced pain and that activated spinal microglia play a direct role in spinal nociceptive processing...
  17. pmc Phase II study of sorafenib in patients with metastatic or recurrent sarcomas
    Robert G Maki
    Melanoma Sarcoma Program, Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Ave, Howard 909, New York, NY 10065, USA
    J Clin Oncol 27:3133-40. 2009
    ..Further evaluation of sorafenib in these and possibly other sarcoma subtypes appears warranted, presumably in combination with cytotoxic or kinase-specific agents...
  18. doi Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors
    Patricia M LoRusso
    Karmanos Cancer Institute, Detroit, Michigan Johns Hopkins University, Baltimore, Maryland, USA
    Clin Cancer Res 17:2502-11. 2011
    ..This phase I trial assessed GDC-0449 treatment in patients with solid tumors refractory to current therapies or for which no standard therapy existed...
  19. ncbi Clinical pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor dabigatran etexilate
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Biberach, Germany
    Clin Pharmacokinet 47:285-95. 2008
    ....
  20. doi Randomized, placebo-controlled, phase III study of oxaliplatin, fluorouracil, and leucovorin with or without PTK787/ZK 222584 in patients with previously treated metastatic colorectal adenocarcinoma
    Eric Van Cutsem
    Digestive Oncology Unit, University Hospital Gasthuisberg, Herestraat 49, 3000 Leuven, Belgium
    J Clin Oncol 29:2004-10. 2011
    ..PTK787/ZK 222584 (PTK/ZK) is a novel oral angiogenesis inhibitor with therapeutic potential for the treatment of solid tumors...
  21. pmc The GLI genes as the molecular switch in disrupting Hedgehog signaling in colon cancer
    Tapati Mazumdar
    Department of Cancer Biology, Lerner Research Institute, Cleveland Clinic, Cleveland, OH 44195, USA
    Oncotarget 2:638-45. 2011
    ....
  22. doi Randomized, placebo-controlled, phase III study of first-line oxaliplatin-based chemotherapy plus PTK787/ZK 222584, an oral vascular endothelial growth factor receptor inhibitor, in patients with metastatic colorectal adenocarcinoma
    J Randolph Hecht
    David Geffen School of Medicine at University of California, Los Angeles, Santa Monica, CA 90404, USA
    J Clin Oncol 29:1997-2003. 2011
    ....
  23. pmc Blocking Hedgehog survival signaling at the level of the GLI genes induces DNA damage and extensive cell death in human colon carcinoma cells
    Tapati Mazumdar
    Department of Cancer Biology, Lerner Research Institute, Cleveland Clinic, Cleveland, Ohio, USA
    Cancer Res 71:5904-14. 2011
    ..Taken together, these findings establish that inhibition of HH signaling at the level of the GLI genes downstream of Smo is critical in the induction of DNA damage in early S-phase, leading to cell death in human colon carcinoma cells...
  24. ncbi Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Gothenburg, Sweden
    Lancet 370:949-56. 2007
    ..After hip replacement surgery, prophylaxis following discharge from hospital is recommended to reduce the risk of venous thromboembolism. Our aim was to assess the oral, direct thrombin inhibitor dabigatran etexilate for such prophylaxis...
  25. pmc Drugging the PI3 kinome: from chemical tools to drugs in the clinic
    Paul Workman
    Cancer Research UK Centre for Cancer Therapeutics, Section of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom
    Cancer Res 70:2146-57. 2010
    ..The challenges and outlook for drugging the PI3 kinome are discussed in the more general context of the role of structural biology and chemical biology in innovative drug discovery...
  26. doi Dabigatran versus warfarin in the treatment of acute venous thromboembolism
    Sam Schulman
    Department of Medicine, McMaster University and Henderson Research Centre, Hamilton, ON, Canada
    N Engl J Med 361:2342-52. 2009
    ..The direct oral thrombin inhibitor dabigatran has a predictable anticoagulant effect and may be an alternative therapy to warfarin for patients who have acute venous thromboembolism...
  27. ncbi Phase II study of sorafenib in patients with advanced hepatocellular carcinoma
    Ghassan K Abou-Alfa
    Memorial Sloan Kettering Cancer Center, York, NY 10022, USA
    J Clin Oncol 24:4293-300. 2006
    ..This phase II study of sorafenib, an oral multikinase inhibitor that targets Raf kinase and receptor tyrosine kinases, assessed efficacy, toxicity, pharmacokinetics, and biomarkers in advanced hepatocellular carcinoma (HCC) patients...
  28. doi Rationale and design of RE-LY: randomized evaluation of long-term anticoagulant therapy, warfarin, compared with dabigatran
    Michael D Ezekowitz
    Lankenau Institute for Medical Research and The Heart Center, Wynnewood, PA, USA
    Am Heart J 157:805-10, 810.e1-2. 2009
    ..The worldwide site distribution and broad range of stroke risk further increase the general applicability of the trial. Results are expected in 2009...
  29. pmc Phase II trial of sorafenib in metastatic thyroid cancer
    Richard T Kloos
    Ohio State University, Department of Internal Medicine, Molecular Virology, Immunology, and Genetics, Pathology, Radiology, Center for Biostatistics, Ohio State University, Columbus, OH 43210, USA
    J Clin Oncol 27:1675-84. 2009
    ..Based on the pivotal role of Ras-Raf-MAP-ERK signaling and vascular endothelial growth factor (VEGF) in papillary thyroid cancer (PTC), we conducted a phase II clinical trial of sorafenib targeting RAF and VEGF receptor kinases in PTC...
  30. ncbi p38 mitogen-activated protein kinase is activated after a spinal nerve ligation in spinal cord microglia and dorsal root ganglion neurons and contributes to the generation of neuropathic pain
    Shan Xue Jin
    Neural Plasticity Research Group, Department of Anesthesia and Critical Care, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02129, USA
    J Neurosci 23:4017-22. 2003
    ..Coactivation of p38 in DRG neurons and spinal microglia may contribute to later phases of neuropathic pain...
  31. ncbi The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans
    Stefan Blech
    Boehringer Ingelheim Pharma GmbH and Co KG, Department of Drug Metabolism and Pharmacokinetics, Biberach, Germany
    Drug Metab Dispos 36:386-99. 2008
    ..o. administration of dabigatran etexilate and that the potential for clinically relevant interactions between dabigatran and drugs metabolized by cytochrome P450 is low...
  32. ncbi Mutant V599EB-Raf regulates growth and vascular development of malignant melanoma tumors
    Arati Sharma
    Department of Pharmacology, Pennsylvania State University College of Medicine, Hershey 17033, USA
    Cancer Res 65:2412-21. 2005
    ..Thus, these studies identify the mechanistic underpinnings by which mutant (V599E)B-RAF promotes melanoma development and show the effectiveness of targeting this protein to inhibit melanoma tumor growth...
  33. doi Cost-effectiveness of dabigatran etexilate for the prevention of stroke and systemic embolism in atrial fibrillation: a Canadian payer perspective
    S V Sorensen
    United BioSource Corporation, Bethesda, Maryland, USA
    Thromb Haemost 105:908-19. 2011
    ..This study demonstrates that dabigatran etexilate is a highly cost-effective alternative to current care for the prevention of stroke and systemic embolism among Canadian AF patients...
  34. pmc The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Ingelheim, Germany
    Br J Clin Pharmacol 64:292-303. 2007
    ..Two double-blind, randomized trials were undertaken to investigate the pharmacokinetics (PK), pharmacodynamics (PD) and tolerability of orally administered dabigatran etexilate in healthy male subjects...
  35. ncbi A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
    J C Lee
    Department of Cellular Biochemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406
    Nature 372:739-46. 1994
    ..Binding of the pyridinyl-imidazole compounds inhibited CSBP kinase activity and could be directly correlated with their ability to inhibit cytokine production, suggesting that the CSBPs are critical for cytokine production...
  36. ncbi Sorafenib induces apoptosis and autophagy in prostate cancer cells in vitro
    Anders Ullen
    Department of Oncology Pathology, Cancer Centrum Karolinska, Karolinska Institutet, 17176 Stockholm, Sweden
    Int J Oncol 37:15-20. 2010
    ....
  37. doi Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma
    Brian I Rini
    Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Ave, Desk R35, Cleveland, OH 44195, USA
    J Clin Oncol 27:4462-8. 2009
    ....
  38. doi Clazosentan to overcome neurological ischemia and infarction occurring after subarachnoid hemorrhage (CONSCIOUS-1): randomized, double-blind, placebo-controlled phase 2 dose-finding trial
    R Loch MacDonald
    St Michael s Hospital, Division of Neurosurgery, Toronto, Ontario, Canada
    Stroke 39:3015-21. 2008
    ....
  39. pmc Preferential binding of a G-quadruplex ligand to human chromosome ends
    Christine Granotier
    LRP, DRR, CEA 92265, Fontenay aux Roses, France
    Nucleic Acids Res 33:4182-90. 2005
    ..They support the hypothesis that G-quadruplex ligands induce and/or stabilize G-quadruplex structures at telomeres of human cells...
  40. doi Dabigatran compared with warfarin in patients with atrial fibrillation and previous transient ischaemic attack or stroke: a subgroup analysis of the RE-LY trial
    Hans Christoph Diener
    Department of Neurology, University Hospital Essen, Essen, Germany
    Lancet Neurol 9:1157-63. 2010
    ..We aimed to assess the effects of dabigatran compared with warfarin in the subgroup of patients with previous stroke or transient ischaemic attack...
  41. ncbi Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma
    James G Christensen
    Department of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, 10724 Science Center Drive, La Jolla, CA 92121, USA
    Mol Cancer Ther 6:3314-22. 2007
    ..Collectively, these data illustrate the potential clinical utility of inhibitors of NPM-ALK in treatment of patients with ALK-positive ALCL...
  42. pmc Hedgehog signaling drives cellular survival in human colon carcinoma cells
    Tapati Mazumdar
    Department of Cancer Biology, Lerner Research Institute, Cleveland Clinic, Cleveland, Ohio 44195, USA
    Cancer Res 71:1092-102. 2011
    ..Collectively, these results highlight the importance of Gli activation downstream of Smo as a therapeutic target in models of human colon carcinoma...
  43. pmc Tonic inhibition in mouse hippocampal CA1 pyramidal neurons is mediated by alpha5 subunit-containing gamma-aminobutyric acid type A receptors
    Valerie B Caraiscos
    Institute of Medical Science, Department of Anesthesia, University of Toronto, Toronto, ON, Canada M5S 1A8
    Proc Natl Acad Sci U S A 101:3662-7. 2004
    ....
  44. doi Indirect comparisons of new oral anticoagulant drugs for efficacy and safety when used for stroke prevention in atrial fibrillation
    Gregory Y H Lip
    University of Birmingham Centre for Cardiovascular Sciences, City Hospital, Birmingham, UK
    J Am Coll Cardiol 60:738-46. 2012
    ..This study sought to perform an indirect comparison analysis of dabigatran etexilate (2 doses), rivaroxaban, and apixaban for their relative efficacy and safety against each other...
  45. ncbi Dabigatran with or without concomitant aspirin compared with warfarin alone in patients with nonvalvular atrial fibrillation (PETRO Study)
    Michael D Ezekowitz
    Lankenau Institute for Medical Research and The Heart Center, Wynnewood, PA, USA
    Am J Cardiol 100:1419-26. 2007
    ..The 2 highest doses of dabigatran suppress D-dimer concentrations. Serious liver toxicity was not seen. The significance of the increase of DTB2 concentrations in dabigatran-treated patients needs resolution...
  46. ncbi Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts
    David W Fry
    Cancer Pharmacology, Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Mol Cancer Ther 3:1427-38. 2004
    ..The results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors...
  47. ncbi A phase II study of sorafenib in patients with chemo-naive castration-resistant prostate cancer
    K N Chi
    Department of Medical Oncology, Vancouver Centre, BC Cancer Agency, Vancouver, British Columbia
    Ann Oncol 19:746-51. 2008
    ..The purpose of this trial was to evaluate the antitumor activity of sorafenib, a multikinase inhibitor of cell proliferation and angiogenesis, in patients with castration-resistant prostate cancer...
  48. doi An autodissemination station for the transfer of an insect growth regulator to mosquito oviposition sites
    R Gaugler
    Center for Vector Biology, Rutgers University, 180 Jones Avenue, New Brunswick, NJ 08901 8536, U S A
    Med Vet Entomol 26:37-45. 2012
    ..Key autodissemination station features include lack of maintenance requirements, biodegradable construction, low cost and low risk...
  49. ncbi Sorafenib (BAY 43-9006) inhibits tumor growth and vascularization and induces tumor apoptosis and hypoxia in RCC xenograft models
    Yong S Chang
    Department of Protein Therapeutics, Bayer Research Center, Bayer HealthCare, Pharmaceuticals, 400 Morgan Lane, West Haven, CT 06516, USA
    Cancer Chemother Pharmacol 59:561-74. 2007
    ..The effect of sorafenib on tumor growth and tumor histology was assessed in both ectopic and orthotopic mouse models of RCC...
  50. ncbi Safety, pharmacokinetics, and preliminary antitumor activity of sorafenib: a review of four phase I trials in patients with advanced refractory solid tumors
    Dirk Strumberg
    Department of Hematology and Medical Oncology, Marienhospital Herne, University Medical School of Bochum, Herne, Germany
    Oncologist 12:426-37. 2007
    ..Based on these findings, continuous daily 400 mg bid sorafenib was chosen as the optimal regimen for phase II/III studies. Trials are ongoing in renal cell carcinoma, hepatocellular carcinoma, melanoma, and non-small cell lung cancer...
  51. doi Double-blind randomized phase II study of the combination of sorafenib and dacarbazine in patients with advanced melanoma: a report from the 11715 Study Group
    David F McDermott
    Division of Hematology Oncology, Beth Israel Deaconess Medical Center, 330 Brookline Ave, East KS 159, Boston, MA, USA
    J Clin Oncol 26:2178-85. 2008
    ..This phase II study evaluated the efficacy and safety of sorafenib plus dacarbazine in patients with advanced melanoma...
  52. ncbi An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms
    Helen Y Zou
    Departments of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, La Jolla, California 92121, USA
    Cancer Res 67:4408-17. 2007
    ..Collectively, these results show the therapeutic potential of targeting c-Met with selective small-molecule inhibitors for the treatment of human cancers...
  53. pmc Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2
    Kevin J French
    Apogee Biotechnology Corporation, Hummelstown, PA 17036, USA
    J Pharmacol Exp Ther 333:129-39. 2010
    ..Therefore, this newly developed SK2 inhibitor provides an orally available drug candidate for the treatment of cancer and other diseases...
  54. doi Validation of an HPLC-UV method for sorafenib determination in human plasma and application to cancer patients in routine clinical practice
    B Blanchet
    Laboratoire de Pharmacologie Toxicologie, Service de Pharmacie, France
    J Pharm Biomed Anal 49:1109-14. 2009
    ..Finally, large interindividual variability and higher exposure in patients experiencing severe toxicity support the need for therapeutic drug monitoring to ensure an optimal exposure to sorafenib...
  55. ncbi Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents
    W P Spooren
    Novartis Pharma AG, Nervous System Research, Basel, Switzerland
    J Pharmacol Exp Ther 295:1267-75. 2000
    ..5 mg/kg) locomotor activity in mice and prepulse inhibition in rats (1, 3, or 10 mg/kg). Thus, these findings indicate that MPEP exhibits anxiolytic-like effects and low risks for sedation and psychotomimetic side-effects in rodents...
  56. pmc The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine
    Michael C Montana
    Washington University Pain Center, Department of Anesthesiology, 660 S Euclid Ave, St Louis, MO 63110, USA
    J Pharmacol Exp Ther 330:834-43. 2009
    ..These results demonstrate that fenobam is analgesic in mice and has an improved in vivo selectivity for mGlu5 over MPEP...
  57. ncbi A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo
    A Iwamaru
    Department of Neurosurgery, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Oncogene 26:2435-44. 2007
    ..We conclude that WP1066 holds promise as a therapeutic agent against malignant gliomas...
  58. doi Safety and efficacy results of the advanced renal cell carcinoma sorafenib expanded access program in North America
    Walter M Stadler
    Department of Medicine, University of Chicago Medical Center, Chicago, Illinois
    Cancer 116:1272-80. 2010
    ..The Advanced Renal Cell Carcinoma Sorafenib (ARCCS) program made sorafenib available to patients with advanced renal cell carcinoma (RCC) before regulatory approval...
  59. ncbi Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5
    Li Liu
    Department of Cancer Biology, Bayer HealthCare Pharmaceuticals, West Haven, Connecticut 06516, USA
    Cancer Res 66:11851-8. 2006
    ....
  60. ncbi A ROCK inhibitor permits survival of dissociated human embryonic stem cells
    Kiichi Watanabe
    Organogenesis and Neurogenesis Group, Center for Developmental Biology, RIKEN, Kobe 650 0047, Japan
    Nat Biotechnol 25:681-6. 2007
    ..We demonstrate that the protective ability of Y-27632 enables SFEB-cultured hES cells to survive and differentiate into Bf1(+) cortical and basal telencephalic progenitors, as do SFEB-cultured mouse ES cells...
  61. doi Sorafenib, but not sunitinib, affects function of dendritic cells and induction of primary immune responses
    Madeleine M Hipp
    Department of Hematology, Oncology and Immunology, University of Tubingen, Tubingen, Germany
    Blood 111:5610-20. 2008
    ..These results indicate that sunitinib, but not sorafenib, is suitable for combination with immunotherapeutic approaches for treatment of cancer patients...
  62. ncbi Efficacy of pyriproxyfen-treated nets in sterilizing and shortening the longevity of Anopheles gambiae (Diptera: Culicidae)
    Kazunori Ohashi
    Health and Crop Sciences Research Laboratory, Sumitomo Chemical Company, Ltd, Hyogo 665 8555, Japan
    J Med Entomol 49:1052-8. 2012
    ....
  63. pmc A clinical phase II study with sorafenib in patients with progressive hormone-refractory prostate cancer: a study of the CESAR Central European Society for Anticancer Drug Research-EWIV
    S Steinbild
    Tumor Biology Center, Albert Ludwigs University Freiburg Freiburg, Germany
    Br J Cancer 97:1480-5. 2007
    ..Sorafenib has antitumour activity in HRPCP when evaluated for RECIST- and PSA-based response. Further investigation as a component of combination regimens is necessary to evaluate its definite or overall clinical benefit for HRPCP...
  64. pmc Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study
    D Strumberg
    Department of Hematology and Medical Oncology, University of Bochum, Marienhospital Herne, Hölkeskampring 40, D 44625 Herne, Germany
    Br J Cancer 106:1722-7. 2012
    ..In a phase I dose-escalation study, regorafenib demonstrated tolerability and antitumour activity in solid tumour patients. The study was expanded to focus on patients with metastatic colorectal cancer (CRC)...
  65. doi Novel 1,2,4-triazolo[1,5-a]pyridines and their fused ring systems attenuate oxidative stress and prolong lifespan of Caenorhabiditis elegans
    Ramadan Ahmed Mekheimer
    Department of Chemistry, Faculty of Science for Girls, King Abdulaziz University, Jeddah, P O Box 50918, Jeddah 21533, Saudi Arabia
    J Med Chem 55:4169-77. 2012
    ..elegans in a dose-dependent manner. Furthermore, treatment of worms with compound 13 was found to significantly attenuate the formation of advanced glycation end products and malondialdehyde in a dose-dependent manner...
  66. doi A phase I dose-escalation study of regorafenib (BAY 73-4506), an inhibitor of oncogenic, angiogenic, and stromal kinases, in patients with advanced solid tumors
    Klaus Mross
    Tumour Biology Center, University Hospital, Freiburg, Germany
    Clin Cancer Res 18:2658-67. 2012
    ..This first-in-man, phase I dose-escalation study assessed the safety, pharmacokinetic, pharmacodynamic, and efficacy profiles of regorafenib in patients with advanced solid tumors...
  67. doi Dabigatran etexilate for stroke prevention in patients with atrial fibrillation: resolving uncertainties in routine practice
    Menno V Huisman
    Department of Thrombosis and Haemostasis, Leiden University Medical Center, Leiden, The Netherlands
    Thromb Haemost 107:838-47. 2012
    ..In addition, cut-off values for different coagulation assay results associated with an increased risk of bleeding are given...
  68. pmc Allosteric drugs: the interaction of antitumor compound MKT-077 with human Hsp70 chaperones
    Aikaterini Rousaki
    Program in Biophysics, The University of Michigan, Ann Arbor, MI 48109, USA
    J Mol Biol 411:614-32. 2011
    ..Suggestions for the improvement of the compound's properties are made on the basis of the binding location and pose...
  69. doi Dissociation of vasospasm and secondary effects of experimental subarachnoid hemorrhage by clazosentan
    Mohammed Sabri
    Division of Neurosurgery, St Michael s Hospital, University of Toronto, 30 Bond Street, Toronto, Ontario, Canada, M5B 1W8
    Stroke 42:1454-60. 2011
    ....
  70. doi Sorafenib induces cell death in chronic lymphocytic leukemia by translational downregulation of Mcl-1
    S Huber
    Third Department of Medicine, Technical University, Munich, Germany
    Leukemia 25:838-47. 2011
    ..Conclusively, sorafenib is highly active in CLL and may compose a new therapeutic option for patients who relapse after immunochemotherapy...
  71. doi Treatments for stroke prevention in atrial fibrillation: a network meta-analysis and indirect comparisons versus dabigatran etexilate
    Neil S Roskell
    Neil Roskell, RTI Health Solutions, Williams House, Manchester Science Park, Lloyd Street North, Manchester M15 6SE, UK
    Thromb Haemost 104:1106-15. 2010
    ..There was no indication of increased intracranial or extracranial haemorrhage with dabigatran etexilate compared to antiplatelet agents...
  72. pmc Ras pathway activation in hepatocellular carcinoma and anti-tumoral effect of combined sorafenib and rapamycin in vivo
    Pippa Newell
    Mount Sinai Liver Cancer Program, Mount Sinai School of Medicine, 1425 Madison Avenue, New York, NY 10029, USA
    J Hepatol 51:725-33. 2009
    ..We investigated the molecular alterations of the Ras pathway in HCC and the antineoplastic effects of sorafenib in combination with rapamycin, an inhibitor of mTOR pathway, in experimental models...
  73. pmc FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML
    Keith W Pratz
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
    Blood 115:1425-32. 2010
    ..These results have important implications for the potential therapeutic use of FLT3 inhibitors in that patients with newly diagnosed FLT3-mutant AML might be less likely to respond clinically to highly selective FLT3 inhibition...
  74. doi Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial
    Axel Grothey
    Division of Medical Oncology, Mayo Clinic, Rochester, MN, USA
    Lancet 381:303-12. 2013
    ..An international phase 3 trial was done to assess the multikinase inhibitor regorafenib in these patients...
  75. doi A comparison of dabigatran etexilate with warfarin in patients with mechanical heart valves: THE Randomized, phase II study to evaluate the safety and pharmacokinetics of oral dabigatran etexilate in patients after heart valve replacement (RE-ALIGN)
    Frans Van de Werf
    University Hospitals Leuven, Department of Cardiovascular Medicine, Leuven, Belgium
    Am Heart J 163:931-937.e1. 2012
    ..Vitamin K antagonists are the only oral anticoagulants approved for long-term treatment of patients with a cardiac valve replacement...
  76. ncbi Structure-based design of novel potent nonpeptide thrombin inhibitors
    Norbert H Hauel
    Boehringer Ingelheim Pharma KG, Research Division, Birkendorfer Strasse 65, D 88397 Biberach Riss, Germany
    J Med Chem 45:1757-66. 2002
    ..This zwitterionic molecule was converted into the double-prodrug 31 (BIBR 1048), which showed strong oral activity in different animal species. On the basis of these results, 31 was chosen for clinical development...
  77. doi Once-daily atazanavir/ritonavir versus twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 48 week efficacy and safety results of the CASTLE study
    Jean Michel Molina
    Department of Infectious Diseases, Saint Louis Hospital, AP HP, Paris University of Paris Diderot, Paris 7, France
    Lancet 372:646-55. 2008
    ..We compared these two combinations directly in treatment-naive patients...
  78. pmc Crizotinib in ALK-rearranged inflammatory myofibroblastic tumor
    James E Butrynski
    Dana Farber Cancer Institute, Boston, MA 02115, USA
    N Engl J Med 363:1727-33. 2010
    ..Funded by Pfizer and others; ClinicalTrials.gov number, NCT00585195.)...
  79. pmc The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers
    Takaaki Sasaki
    Lowe Center for Thoracic Oncology, Dana Farber Cancer Institute, D820, 44 Binney Street, Boston, MA 02115, USA
    Cancer Res 70:10038-43. 2010
    ..Our findings highlight the importance of studying drug resistance mechanisms in order to develop effective clinical treatments for patients with ALK-translocated cancers...
  80. pmc Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK
    Ryohei Katayama
    Massachusetts General Hospital Cancer Center, Boston, MA 02129, USA
    Proc Natl Acad Sci U S A 108:7535-40. 2011
    ..Thus, we have developed a model of acquired resistance to ALK inhibitors and have shown that second-generation ALK TKIs or Hsp90 inhibitors are effective in treating crizotinib-resistant tumors harboring secondary gatekeeper mutations...
  81. doi Biomarkers predicting outcome in patients with advanced renal cell carcinoma: Results from sorafenib phase III Treatment Approaches in Renal Cancer Global Evaluation Trial
    Carol Pena
    Bayer HealthCare Pharmaceuticals, Montville, New Jersey 07045 1000, USA
    Clin Cancer Res 16:4853-63. 2010
    ....
  82. pmc Behavioral and functional evidence of metabotropic glutamate receptor 2/3 and metabotropic glutamate receptor 5 dysregulation in cocaine-escalated rats: factor in the transition to dependence
    Yue Hao
    Molecular and Integrative Neurosciences Department, The Scripps Research Institute, La Jolla, California, USA
    Biol Psychiatry 68:240-8. 2010
    ..We examined here whether neuroadaptive dysregulation of metabotropic glutamate receptor function is a factor in escalating cocaine self-administration...
  83. pmc Repetitive self-grooming behavior in the BTBR mouse model of autism is blocked by the mGluR5 antagonist MPEP
    Jill L Silverman
    Laboratory of Behavioral Neuroscience, National Institute of Mental Health, Porter Neuroscience Research Center, Bethesda, MD 20892, USA
    Neuropsychopharmacology 35:976-89. 2010
    ..Our findings suggest that antagonists of mGluR5 receptors may have selective therapeutic efficacy in treating repetitive behaviors in autism...
  84. doi Sorafenib for the treatment of unresectable hepatocellular carcinoma
    Robert C Kane
    Office of Oncology Drug Products, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, MD 20993 0004, USA
    Oncologist 14:95-100. 2009
    ..Montville, NJ, and Onyx Pharmaceuticals Corp., Emeryville, CA), an oral kinase inhibitor, for the treatment of patients with unresectable hepatocellular carcinoma (HCC)...
  85. pmc p38 MAPK links oxidative stress to autophagy-related gene expression in cachectic muscle wasting
    J M McClung
    Exercise Biochemistry Laboratory, University of Florida, Gainesville, Florida, USA
    Am J Physiol Cell Physiol 298:C542-9. 2010
    ....
  86. pmc Inhibition of the p38 kinase suppresses the proliferation of human ER-negative breast cancer cells
    Lu Chen
    Breast Center, Baylor College of Medicine, Houston, Texas 77030, USA
    Cancer Res 69:8853-61. 2009
    ..Because most ER-negative breast tumors express mutant p53, our results provide the foundation for future development of p38 inhibitors to target p38 for the treatment of p53 mutant and ER-negative breast cancers...
  87. doi GDC-0449--targeting the hedgehog signaling pathway
    Christine Dierks
    Department of Hematology and Oncology, Freiburg University Medical Center, Hugstetterstrasse 55, 79106, Freiburg, Germany
    Recent Results Cancer Res 184:235-8. 2010
    ..It was successfully tested in a phase-I clinical trial demonstrating good pharmacodynamic (PD) and pharmacokinetic (PK) properties and showing objective response and clinical benefit in several patients with basal cell carcinoma...
  88. doi Ibudilast in relapsing-remitting multiple sclerosis: a neuroprotectant?
    F Barkhof
    Department of Radiology, VU University Medical Center, MB, Amsterdam, The Netherlands
    Neurology 74:1033-40. 2010
    ..This study evaluated the safety, tolerability, and effects on MRI parameters of 2 different doses of ibudilast in relapsing forms of MS...
  89. ncbi Nicotinic acetylcholine receptors: an overview on drug discovery
    Dieter D'Hoedt
    Department of Neurosciences, CMU, Geneve, Switzerland
    Expert Opin Ther Targets 13:395-411. 2009
    ..Results/conclusion: Long-standing efforts in this field should soon result in the finding of new molecules that might be applicable to situations ranging from neurological diseases to immune treatments...
  90. doi Sorafenib inhibits the shedding of major histocompatibility complex class I-related chain A on hepatocellular carcinoma cells by down-regulating a disintegrin and metalloproteinase 9
    Keisuke Kohga
    Department of Gastroenterology and Hepatology, Osaka University Graduate School of Medicine, Osaka, Japan
    Hepatology 51:1264-73. 2010
    ..Conclusion: ADAM9 is involved in MICA ectodomain shedding in HCC cells, and sorafenib can modulate ADAM9 expression. Sorafenib therapy may have a previously unrecognized effect on antitumor immunity in patients with HCC...
  91. doi Upfront, randomized, phase 2 trial of sorafenib versus sorafenib and low-dose interferon alfa in patients with advanced renal cell carcinoma: clinical and biomarker analysis
    Eric Jonasch
    Department of Genitourinary Medical Oncology, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Cancer 116:57-65. 2010
    ..The objective of this study was to independently evaluate the objective response rate of sorafenib and sorafenib plus low-dose interferon-alfa 2b (IFN) as frontline therapy in patients with metastatic renal cell carcinoma (mRCC)...
  92. ncbi A phase I and pharmacokinetic study of the mitochondrial-specific rhodacyanine dye analog MKT 077
    C D Britten
    Cancer Therapy and Research Center, Institute for Drug Development, and The University of Texas Health Science Center at San Antonio, 78229, USA
    Clin Cancer Res 6:42-9. 2000
    ....
  93. doi Effect of ROCK inhibitor Y-27632 on normal and variant human embryonic stem cells (hESCs) in vitro: its benefits in hESC expansion
    Kalamegam Gauthaman
    Department of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of Singapore, 5 Lower Kent Ridge Road, Singapore, 119074, Singapore
    Stem Cell Rev 6:86-95. 2010
    ..The results confirmed that Y-27632 is a useful agent that aids in the expansion of undifferentiated hESC numbers for downstream applications in regenerative medicine...
  94. ncbi Effects of mGlu1 and mGlu5 receptor antagonists on negatively reinforced learning
    A Gravius
    Preclinical R and D, Merz Pharmaceuticals, Frankfurt am Main, Germany
    Behav Pharmacol 16:113-21. 2005
    ..5 and 5 mg/kg inhibited fear conditioning in the FPS when tested 24 h later. In contrast, EMQMCM was ineffective. Our findings suggest diverse involvement of mGlu1 and mGlu5 receptors in negatively reinforced learning...
  95. ncbi Chloropyridinyl neonicotinoid insecticides: diverse molecular substituents contribute to facile metabolism in mice
    Kevin A Ford
    Environmental Chemistry and Toxicology Laboratory, Department of Environmental Science, Policy and Management, University of California, Berkeley, 94720 3112, USA
    Chem Res Toxicol 19:944-51. 2006
  96. doi Presence of a ROCK inhibitor in extracellular matrix supports more undifferentiated growth of feeder-free human embryonic and induced pluripotent stem cells upon passaging
    Mohammad Pakzad
    Department of Stem Cells and Developmental Biology, Royan Institute for Stem Cell Biology and Technology, ACECR, P O Box 19395 4644, Tehran, Iran
    Stem Cell Rev 6:96-107. 2010
    ..This is due not only to an anti-apoptotic effect, but also to an increase in the ECM-cells interaction. Therefore, we believe this method will be useful for both current and future applications of these pluripotent stem cells...
  97. pmc Myosin light chain kinase activation and calcium sensitization in smooth muscle in vivo
    Yusuke Mizuno
    Dept Physiology, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9040, USA
    Am J Physiol Cell Physiol 295:C358-64. 2008
    ..Thus the onset of agonist-induced contraction in phasic smooth muscle results from the rapid and coordinated activation of MLCK with hierarchical inhibition of MLCP by CPI-17 and MYPT1 phosphorylation...
  98. ncbi Sphingosine 1-phosphate stimulates smooth muscle cell differentiation and proliferation by activating separate serum response factor co-factors
    Kashelle Lockman
    Department of Pathology and Laboratory Medicine, University of North Carolina, Chapel Hill, North Carolina 27599, USA
    J Biol Chem 279:42422-30. 2004
    ..Taken together these results demonstrate that S1P activates multiple signaling pathways in SMC and regulates proliferation by ERK-dependent activation of Elk-1 and differentiation by RhoA-dependent activation of MRTF-A...
  99. ncbi NMR-spectroscopy-based metabonomic approach to the analysis of Bay41-4109, a novel anti-HBV compound, induced hepatotoxicity in rats
    Chang Shi
    Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, PR China
    Toxicol Lett 173:161-7. 2007
    ..The application of (1)H NMR spectroscopy to an array of biological samples comprising urine, serum and liver tissue extracts yields new insight into the hepatotoxicity of xenobiotics...
  100. ncbi NO-independent stimulators of soluble guanylate cyclase
    A Straub
    Institute of Medicinal Chemistry, Pharma Research Centre, Bayer AG, Wuppertal, FRG
    Bioorg Med Chem Lett 11:781-4. 2001
    ..Several pyrazolopyridinylpyrimidines are shown to relax aortic rings and revealed a long-lasting blood pressure lowering effect in rats after oral application...
  101. ncbi NO-independent regulatory site on soluble guanylate cyclase
    J P Stasch
    Pharma Research Center, Bayer AG, Aprather Wey 18a, D 42096 Wuppertal, Germany
    Nature 410:212-5. 2001
    ..This results in antiplatelet activity, a strong decrease in blood pressure and an increase in survival in a low-NO rat model of hypertension, and as such may offer an approach for treating cardiovascular diseases...

Research Grants71

  1. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2007
    ..libraries of indoles, benzofurans, benzopyrans, coumarins, isocoumarins, phthalides, pyrones, 2-quinolones, pyridines, isoquinolin-1-ones, isoindolin-1-ones, isoquinolines, carbolines, isoindolo[2,1-a]indoles, carbazoles, ..
  2. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  3. Au/Pt Catalysis in the Synthesis of Elaborate N-Heterocycles: Methodology Develop
    Liming Zhang; Fiscal Year: 2009
    ..g., pyridines, pyrroles, oxazoles, pyrroline and indoles)...
  4. Au/Pt Catalysis in the Synthesis of Elaborate N-Heterocycles: Methodology Develop
    Liming Zhang; Fiscal Year: 2010
    ..g., pyridines, pyrroles, oxazoles, pyrroline and indoles)...
  5. Carbon-Carbon Bond Forming Reactions Via C-H Activation
    Jonathan A Ellman; Fiscal Year: 2011
    ..will provide 1,2-dihydropyridines, which are extremely versatile intermediates in the synthesis of pyridines and piperidines...
  6. Carbon-Carbon Bond Forming Reactions Via C-H Activation
    Jonathan A Ellman; Fiscal Year: 2010
    ..will provide 1,2-dihydropyridines, which are extremely versatile intermediates in the synthesis of pyridines and piperidines...
  7. Carbon-Carbon Bond Forming Reactions Via C-H Activation
    JONATHAN ELLMAN; Fiscal Year: 2009
    ..will provide 1,2-dihydropyridines, which are extremely versatile intermediates in the synthesis of pyridines and piperidines...
  8. Approaches to Bioactive Aminoimidazole Natural Products
    CARL LOVELY; Fiscal Year: 2007
    ..Also, it is planned to establish the applicability of the rearrangement to imidazo[4,5-b]pyridines, if successful, the rearranged products might function as key intermediates in approaches to several monomeric ..
  9. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick J Walsh; Fiscal Year: 2010
    ..to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  10. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick Walsh; Fiscal Year: 2007
    ..to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  11. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick J Walsh; Fiscal Year: 2010
    ..to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  12. Synthetic Methods Involving Decarboxylative Coupling
    JON TUNGE; Fiscal Year: 2007
    ..amines, functionally differentiated hexadienes, and various biologically important heterocycles including pyridines, azetidines, and piperidines...
  13. Synthetic Methods Involving Decarboxylative Coupling
    Jon A Tunge; Fiscal Year: 2010
    ..amines, functionally differentiated hexadienes, and various biologically important heterocycles including pyridines, azetidines, and piperidines...
  14. Inhibitor of FtsZ Polymerization in M. tuberculosis
    Robert Reynolds; Fiscal Year: 2004
    ..The 2-alkoxy-carbonylamino-pyridines (2-ACPs) potently inhibit the growth of Mtb with an MIC99 (SRI-3072) as low as 0.15 microgram/ml (0...
  15. Design, Syntheses and Studies of Novel Antituberculosis Agents
    Marvin J Miller; Fiscal Year: 2010
    ..synthesized, potent, non-toxic, remarkably selective small molecule antiTB agents, including imidazo[1,2-a]pyridines, the development of which will be the second goal...
  16. ONCOGENE DIRECTED SYNTHESIS OF CEPHALOSTATIN CANCER DRUG
    Philip Fuchs; Fiscal Year: 2004
    ..the contribution of the central arene moiety to anticancer activity by testing pairs of unsymmetrical annulated pyridines derived from the best simplified hexacyclic steroidal subunits...
  17. Synthesis of (-)-cananodine, an alkaloid active against hepatocellular carcinoma
    JAMES VYVYAN; Fiscal Year: 2007
    ..cross-coupling of alkenyl triflates, alkenyl boronates, or alkylzinc reagents with highly substituted pyridines having complementary functionality; 2) preparation of tetrahydro-5H-cyclohepta[b]pyridine derivatives via an ..
  18. Pyridine Synthesis via an Olefin C-H Alkenylation/Azaelectrocyclization Strategy
    ASHLEY BERMAN; Fiscal Year: 2007
    ..This strategy allows for the concise stereoselective synthesis of pyridines, providing rapid access to this important class of compounds from readily available starting materials...
  19. SYNTHESIS & SYNTHETIC UTILITY OF 1-ACYLDIHYDROPYRIDINES
    DANIEL COMINS; Fiscal Year: 1990
    ..This will allow for development of novel syntheses of substituted pyridines through aromatization of the dihydropyridine intermediates...
  20. THE GASTRIC ACID PUMP AS A TARGET FOR ULCER TREATMENT
    George Sachs; Fiscal Year: 2004
    ..The potential binding sites of SCH28080 and other imidazo-pyridines will be investigated by kinetic measurements in cells transfected with the H+,K+ ATPase and mutated enzyme...
  21. PERICYCLIC REACTIONS FOR ORGANIC SYNTHESIS
    RICK DANHEISER; Fiscal Year: 2001
    ..Heterocyclic variants of this process will be developed leading to substituted pyridines, dihydroisobenzofurans, and isoindoles...
  22. STUDIES IN ALKALOID TOTAL SYNTHESIS
    STEVEN WEINREB; Fiscal Year: 2003
    ..Finally, methodology for regioselective construction of highly substituted pyridines, which are components of the thiostreptone class of antibiotics, will be pursed via an intramolecular hetero ..