indolizines

Summary

Top Publications

  1. ncbi Synthesis of 2,4,6-trisubstituted chiral piperidines and (-)-dendroprimine by one-pot asymmetric azaelectrocyclization protocol
    Toyoharu Kobayashi
    School of Science and Technology, Kwansei Gakuin University, Gakuen 2 1, Sanda, Hyogo 669 1337, Japan
    Org Lett 8:3813-6. 2006
  2. ncbi Abrogation of skin disease in LUPUS-prone MRL/FASlpr mice by means of a novel tylophorine analog
    Jin Young Choi
    Yale School of Medicine, Yale University, New Haven, Connecticut, USA
    Arthritis Rheum 54:3277-83. 2006
  3. ncbi Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases
    Laura Casu
    Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Cagliari, Italy
    Bioorg Med Chem Lett 21:7041-4. 2011
  4. ncbi Tylophorine arrests carcinoma cells at G1 phase by downregulating cyclin A2 expression
    Chia Mao Wu
    Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 350, Taiwan, ROC
    Biochem Biophys Res Commun 386:140-5. 2009
  5. pmc Lycobetaine acts as a selective topoisomerase II beta poison and inhibits the growth of human tumour cells
    H U Barthelmes
    Department of Chemistry, Division of Food Chemistry and Environmental Toxicology, University of Kaiserslautern, Erwin Schroedinger Str 52, 67663 Kaiserslautern, Germany
    Br J Cancer 85:1585-91. 2001
  6. ncbi Indolizines as novel potent inhibitors of 15-lipoxygenase
    Lise Lotte Gundersen
    Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N 0315 Oslo, Norway
    Bioorg Med Chem 11:5409-15. 2003
  7. ncbi Synthesis of N-, S-, and C-glycoside castanospermine analogues with selective neutral alpha-glucosidase inhibitory activity as antitumour agents
    Elena M Sánchez-Fernández
    Instituto de Investigaciones Quimicas, CSIC, Americo Vespucio 49, Isla de la Cartuja, E 41092 Sevilla, Spain
    Chem Commun (Camb) 46:5328-30. 2010
  8. ncbi Inhibition of cell growth and nuclear factor-kappaB activity in pancreatic cancer cell lines by a tylophorine analogue, DCB-3503
    Her Shyong Shiah
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA
    Mol Cancer Ther 5:2484-93. 2006
  9. ncbi Synthesis of indolizine derivatives with selective antibacterial activity against Mycobacterium tuberculosis
    Lise Lotte Gundersen
    Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N 0315 Oslo, Norway
    Eur J Pharm Sci 30:26-35. 2007
  10. ncbi A quantitative structure-activity relationship study on a novel class of calcium-entry blockers: 1-[(4-(aminoalkoxy)phenyl)sulphonyl]indolizines
    S P Gupta
    Department of Chemistry, Birla Institute of Technology and Science, Pilani 333031, India
    Eur J Med Chem 38:867-73. 2003

Detail Information

Publications190 found, 100 shown here

  1. ncbi Synthesis of 2,4,6-trisubstituted chiral piperidines and (-)-dendroprimine by one-pot asymmetric azaelectrocyclization protocol
    Toyoharu Kobayashi
    School of Science and Technology, Kwansei Gakuin University, Gakuen 2 1, Sanda, Hyogo 669 1337, Japan
    Org Lett 8:3813-6. 2006
    ..Based on the method, the asymmetric synthesis of an indolizidine alkaloid, (-)-dendroprimine, was achieved...
  2. ncbi Abrogation of skin disease in LUPUS-prone MRL/FASlpr mice by means of a novel tylophorine analog
    Jin Young Choi
    Yale School of Medicine, Yale University, New Haven, Connecticut, USA
    Arthritis Rheum 54:3277-83. 2006
    ..To test the therapeutic effect of DCB-3503, a synthetic compound derived from a natural product that inhibits NF-kappaB, on end-organ disease in the MRL-Fas(lpr) murine model of systemic lupus erythematosus (SLE)...
  3. ncbi Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases
    Laura Casu
    Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Cagliari, Italy
    Bioorg Med Chem Lett 21:7041-4. 2011
    ..Remarkably, ungeremine was found to largely increments the DNA cleavage promoted by bacterial topoisomerase IA, a new target in antimicrobial chemotherapy...
  4. ncbi Tylophorine arrests carcinoma cells at G1 phase by downregulating cyclin A2 expression
    Chia Mao Wu
    Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 350, Taiwan, ROC
    Biochem Biophys Res Commun 386:140-5. 2009
    ..Thus, we are the first to report that the downregulated cyclin A2 plays a vital role in G1 arrest by tylophorine in carcinoma cells...
  5. pmc Lycobetaine acts as a selective topoisomerase II beta poison and inhibits the growth of human tumour cells
    H U Barthelmes
    Department of Chemistry, Division of Food Chemistry and Environmental Toxicology, University of Kaiserslautern, Erwin Schroedinger Str 52, 67663 Kaiserslautern, Germany
    Br J Cancer 85:1585-91. 2001
    ..It is reasonable to assume that this mechanism will cause or at least contribute significantly to the antitumour activity...
  6. ncbi Indolizines as novel potent inhibitors of 15-lipoxygenase
    Lise Lotte Gundersen
    Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N 0315 Oslo, Norway
    Bioorg Med Chem 11:5409-15. 2003
    ..We have examined 1-substituted indolizines as possible inhibitors of 15-LO from soy beans and from rabbit reticulocytes...
  7. ncbi Synthesis of N-, S-, and C-glycoside castanospermine analogues with selective neutral alpha-glucosidase inhibitory activity as antitumour agents
    Elena M Sánchez-Fernández
    Instituto de Investigaciones Quimicas, CSIC, Americo Vespucio 49, Isla de la Cartuja, E 41092 Sevilla, Spain
    Chem Commun (Camb) 46:5328-30. 2010
    ....
  8. ncbi Inhibition of cell growth and nuclear factor-kappaB activity in pancreatic cancer cell lines by a tylophorine analogue, DCB-3503
    Her Shyong Shiah
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA
    Mol Cancer Ther 5:2484-93. 2006
    ..It is a potentially useful compound in the management of cancers in which cyclin D1 overexpression and high NF-kappaB activity play a pivotal role...
  9. ncbi Synthesis of indolizine derivatives with selective antibacterial activity against Mycobacterium tuberculosis
    Lise Lotte Gundersen
    Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N 0315 Oslo, Norway
    Eur J Pharm Sci 30:26-35. 2007
    1-substituted indolizines with activity against Mycobacterium tuberculosis have been synthesized. The most active compounds carry an hydroxyphenylmethyl- or hydroxyalkyl substituent in the indolizine 1-position...
  10. ncbi A quantitative structure-activity relationship study on a novel class of calcium-entry blockers: 1-[(4-(aminoalkoxy)phenyl)sulphonyl]indolizines
    S P Gupta
    Department of Chemistry, Birla Institute of Technology and Science, Pilani 333031, India
    Eur J Med Chem 38:867-73. 2003
    ..relationship (QSAR) study has been made on two different series of 1-[(4-(aminoalkoxy)phenyl)sulphonyl]indolizines acting as calcium entry blockers, using some physicochemical and structural parameters...
  11. ncbi Indolizine 1-sulfonates as potent inhibitors of 15-lipoxygenase from soybeans
    Solomon Teklu
    Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N 0315 Oslo, Norway
    Bioorg Med Chem 13:3127-39. 2005
    ..The enzyme inhibition was not affected by preincubation or the presence of a detergent and no significant particle formation was observed. Hence, inhibition from aggregates of indolizines, promiscuous inhibition, is highly unlikely.
  12. ncbi The interaction between tylophorine B and TMV RNA
    Zhen Xi
    State Key Laboratory of Elemento Organic Chemistry and Department of Chemical Biology, Nankai University, Tianjin, China
    Bioorg Med Chem Lett 16:4300-4. 2006
    ..This work may shed light on the possible molecular inhibition mechanism against TMV by tylophorine B, and provide clues in rational design of sequence-specific RNA binding antivirus drugs...
  13. ncbi Recent progress in synthesis and bioactivity studies of indolizines
    Girija S Singh
    Chemistry Department, University of Botswana, Private Bag 0022, Gaborone, Botswana
    Eur J Med Chem 46:5237-57. 2011
    ..Consequently this review emphasizes the significant development in synthetic methods of indolizines during the current decade, and the importance of indolizines in drug discovery.
  14. ncbi Glycosidase inhibition by ring-modified castanospermine analogues: tackling enzyme selectivity by inhibitor tailoring
    Matilde Aguilar-Moncayo
    Departamento de Quimica Organica, Facultad de Quimica, Universidad de Sevilla, Profesor García González 1, 41012, Sevilla, Spain
    Org Biomol Chem 7:2738-47. 2009
    ....
  15. ncbi Anti-inflammatory effects of 7-methoxycryptopleurine and structure-activity relations of phenanthroindolizidines and phenanthroquinolizidines
    Cheng Wei Yang
    Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County, Taiwan, ROC
    Biochem Biophys Res Commun 354:942-8. 2007
    ..Moreover, in general, phenanthroquinolizidines are more potent than their respective phenanthroindolizines...
  16. ncbi Novel mode of action of tylophorine analogs as antitumor compounds
    Wenli Gao
    Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, USA
    Cancer Res 64:678-88. 2004
    ..In summary, these tylophorine analogs are a unique class of antitumor compounds that have a mode of action different from known antitumor drugs...
  17. ncbi Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents
    Wenli Gao
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA
    Bioorg Med Chem Lett 17:4338-42. 2007
    ..05 for DCB-3503 and P<0.01 for PA-7). Their potent antitumor activities correlated with their potent NF-kappaB-inhibitory effects and their cyclin D1 down-regulatory effects...
  18. ncbi Selective interaction between tylophorine B and bulged DNA
    Zhen Xi
    State Key Laboratory of Elemento Organic Chemistry and Department of Chemical Biology, Nankai University, Tianjin 300071, China
    Bioorg Med Chem Lett 15:2673-7. 2005
    ..These findings may shed some light on tylophorine B's mode of action in biological systems and result in the rational design of sequence-specific DNA binding molecules...
  19. ncbi Effects of a novel tylophorine analog on collagen-induced arthritis through inhibition of the innate immune response
    Xin You
    Yale University, New Haven, Connecticut 06520 8031, USA
    Arthritis Rheum 54:877-86. 2006
    ..To test the effects of a novel tylophorine analog, DCB 3503, on the prevention and treatment of collagen-induced arthritis (CIA) and to elucidate its underlying mechanisms...
  20. ncbi Phospholipid microspheres: a novel delivery mode for targeting antileishmanial agent in experimental leishmaniasis
    S Medda
    Division of Biomembrane, Indian Institute of Chemical Biology, Calcuta 700032, India
    J Drug Target 11:123-8. 2003
    ..Thus, mannose-grafted microspheres may have possible application in the clinics not only in visceral leishmaniasis, but also in other macrophage-associated disorders...
  21. pmc DCB-3503, a tylophorine analog, inhibits protein synthesis through a novel mechanism
    Ying Wang
    Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, United States of America
    PLoS ONE 5:e11607. 2010
    ..The inhibition of growth leads to cancer cell differentiation instead of cell death. However, the mechanisms of action of tylophorine analogs is unknown...
  22. ncbi Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors
    Andrew F Donnell
    Worldwide Medicinal Chemistry, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 20:2163-7. 2010
    Substituted pyridazino[4,5-b]indolizines were identified as potent and selective PDE4B inhibitors...
  23. ncbi Determining the scope of the organolanthanide-catalyzed, sequential intramolecular amination/cyclization reaction: formation of substituted quinolizidines, indolizidines, and pyrrolizidines
    Gary A Molander
    Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6323, USA
    J Org Chem 68:9214-20. 2003
    ..The sense of relative asymmetric induction was contrary to previously studied systems, and although some questions remain, a rationalization for these results is put forward...
  24. ncbi Asymmetric synthesis of an axially chiral antimitotic biaryl via an atropo-enantioselective Suzuki cross-coupling
    Audrey Herrbach
    Institut de Chimie des Substances Naturelles, CNRS, Avenue de la Terrasse, 91198 Gif sur Yvette, France
    J Org Chem 68:4897-905. 2003
    ..This work gives the first application of the asymmetric Suzuki coupling to a biologically relevant target...
  25. ncbi Synthesis of heteroarenes using cascade radical cyclisation via iminyl radicals
    W Russell Bowman
    Department of Chemistry, Loughborough University, Leicestershire, UK
    Org Biomol Chem 3:1460-7. 2005
    ..The biologically active alkaloids mappicine and luotonin A were synthesised using the new methodology. A novel radical conversion of nitriles to primary amides is proposed...
  26. ncbi Asymmetric total synthesis of (-)-alkaloid 223A and its 6-epimer
    Xiaotao Pu
    State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, China
    J Org Chem 68:4400-5. 2003
    ....
  27. ncbi A flexible approach toward trisubstituted piperidines and indolizidines: synthesis of 6-epi-indolizidine 223A
    Joel M Harris
    Department of Chemistry, Emory University, Atlanta, Georgia 30322, USA
    J Org Chem 68:4371-81. 2003
    ..The structure of the natural 223A alkaloid (5b) differs from that of the epi-isomer 5a synthesized in this study in the configuration at the 6-position of the indolizidine ring...
  28. ncbi Synthesis of putative uniflorine A
    Andrew S Davis
    Department of Chemistry, University of Wollongong, Wollongong, New South Wales, 2522, Australia
    J Org Chem 69:3139-43. 2004
    ..The structure of the final synthetic product was unequivocally determined by single-crystal X-ray study of its pentaacetate derivative. Thus it was concluded that the proposed structure of uniflorine A is incorrect...
  29. ncbi New synthetic approach to enantiopure bicyclic sulfonium salts: swainsonine analogues
    Vanda Cerè
    Department of Organic Chemistry, A Mangini University of Bologna, Viale Risorgimento 4, I 40136 Bologna, Italy
    J Org Chem 68:3311-4. 2003
    ..The synthetic strategy is based on a stereo- and regiospecific transannular cyclization reaction of nine-membered cyclic sulfides, mediated by Me(3)SiI or carried out under acidic catalysis...
  30. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits, 2050, South Africa
    Nat Prod Rep 22:603-26. 2005
  31. ncbi Studies on the biosynthesis of paraherquamide A and VM99955. A theoretical study of intramolecular Diels-Alder cycloaddition
    Luis R Domingo
    Instituto de Ciencia Molecular, Departamento de Quimica Organica, Universidad de Valencia, Dr Moliner 50, E 46100 Burjassot, Valencia, Spain
    J Org Chem 68:2895-902. 2003
    ..The results are in reasonable agreement with the available experimental data...
  32. ncbi One-pot hydrogenation conditions for a sequential process to (+)-monomorine
    Guncheol Kim
    Department of Chemistry, College of Natural Science, Chungnam National University, Taejon 305 764, Korea
    J Org Chem 68:5395-8. 2003
    ..The precursors could be prepared concisely using B-alkyl Suzuki cross coupling of a chiral homoallylamine and a vinyl iodide or an iodofuran derivative...
  33. ncbi Epoxide-initiated cationic cyclization of azides: a novel method for the stereoselective construction of 5-hydroxymethyl azabicyclic compounds and application in the stereo- and enantioselective total synthesis of (+)- and (-)-indolizidine 167B and 209D
    P Ganapati Reddy
    Department of Chemistry, Indian Institute of Technology, Madras, Chennai 600036, India
    J Org Chem 69:3093-101. 2004
    ..Further, the enantioselective total synthesis of natural and unnatural indolizidine alkaloids 167B and 209D was accomplished by using Sharpless asymmetric dihydroxylation as a key step...
  34. ncbi Enantioselective synthesis of (-)-dendroprimine and isomers
    Axelle De Saboulin Bollena
    Departement de Chimie, UMR 6504, CNRS et Université Blaise Pascal Clermont Ferrand, 63177 Aubiere, France
    J Nat Prod 67:1029-31. 2004
    ..The first total synthesis of naturally occurring (-)-dendroprimine has been achieved in five steps...
  35. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits 2050, South Africa
    Nat Prod Rep 20:458-75. 2003
    ..The literature from July 2001 to June 2002 is reviewed, and 142 references are cited...
  36. ncbi Concise enantioselective synthesis of 3,5-dialkyl-substituted indolizidine alkaloids via sequential cross-metathesis-double-reductive cyclization
    Stefan Randl
    Technische Universitat Berlin, Institut fur Chemie, Strasse des 17 Juni 135, D 10623 Berlin, Germany
    J Org Chem 68:8879-82. 2003
    ..Our concept presents one of a few examples of a highly selective CM reaction in the synthesis of a natural product...
  37. ncbi A new synthetic method for an indolizidine skeleton by C-N bond formation via a pi-allylpalladium complex
    Yaeko Yamada
    School of Pharmaceutical Sciences, Kitasato University, Minato ku, Tokyo 108 8641, Japan
    Chem Pharm Bull (Tokyo) 52:1082-5. 2004
    ..These results must be available for syntheses of various functional indolizidine alkaloids...
  38. ncbi New crinine-type alkaloids with inhibitory effect on induction of inducible nitric oxide synthase from Crinum yemense
    Osama Bashir Abdel-Halim
    Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
    J Nat Prod 67:1119-24. 2004
    ..g. 1, (+)-bulbispermine (6), (+)-crinamine (7), (+)-6-hydroxycrinamine (8), and (-)-lycorine (9), showed inhibitory effects on nitric oxide production and induction of inducible nitric oxide synthase...
  39. ncbi Asymmetric, stereocontrolled total synthesis of paraherquamide A
    Robert M Williams
    Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA
    J Am Chem Soc 125:12172-8. 2003
    ..2.2]diazaoctane ring system...
  40. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits 2050, South Africa
    Nat Prod Rep 21:625-49. 2004
    ..The literature from July 2002 to June 2003 is reviewed, and 174 references are cited...
  41. ncbi A pair of epimeric 13-hydroxy-2,3,6,7-tetramethoxy-8b,11,12,12a,13,13a-hexahydro-9H-9a-azacyclopenta[b]triphenylene-10-ones
    Cara Nygren
    Department of Chemistry, University of Tennessee, Knoxville, TN 37996, USA
    Acta Crystallogr C 60:o208-10. 2004
    ..The two molecules in the asymmetric unit of (III) are structurally the same. Compounds (II) and (III) are epimers at the C atom carrying the OH group; otherwise they are very similar in structure...
  42. ncbi Asymmetric total synthesis of dendrobatid alkaloids: preparation of indolizidine 251F and its 3-desmethyl analogue using an intramolecular Schmidt reaction strategy
    Aaron Wrobleski
    Department of Medicinal Chemistry, University of Kansas, Room 4070, Malott Hall, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045 7582, USA
    J Am Chem Soc 126:5475-81. 2004
    ..2.1] --> [3.3.0] skeletal rearrangement to deliver diquinane 4a. In similar fashion, 4a was manipulated to an appropriate keto azide, and an intramolecular Schmidt reaction generated the core cyclic architecture of 251F...
  43. ncbi Palladium-catalyzed asymmetric allylic substitution of 2-arylcyclohexenol derivatives: asymmetric total syntheses of (+)-crinamine, (-)-haemanthidine, and (+)-pretazettine
    Toyoki Nishimata
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060 0812, Japan
    J Org Chem 69:1837-43. 2004
    ..Thus, the asymmetric total synthesis of (+)-crinamine was achieved in 10 steps from 11c, and the overall yield is 19%. The total synthesis of (-)-haemanthidine was also achieved from 9 by a short sequence of steps...
  44. ncbi Studies towards the enantioselective synthesis of 5,6,8-trisubstituted amphibian indolizidine alkaloids via enaminone intermediates
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Johannesburg, P O WITS 2050, South Africa
    Org Biomol Chem 3:836-47. 2005
    ..Several further transformations of these potential scaffolds for the synthesis of the target alkaloidal systems are also reported...
  45. ncbi Enantioselective synthesis of piperidine, indolizidine, and quinolizidine alkaloids from a phenylglycinol-derived delta-lactam
    Mercedes Amat
    Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, Spain
    J Org Chem 68:1919-28. 2003
    ....
  46. ncbi Synthesis and biological evaluation of B-ring analogues of (-)-rhazinilam
    Anne Décor
    Institut de Chimie des Substances Naturelles, CNRS, Avenue de la Terrasse, 91198 Gif sur Yvette Cedex, France
    Bioorg Med Chem 14:2314-32. 2006
    ..A few analogues either active (like 6f) or inactive (like 5o) on tubulin showed significant inhibition of the growth of KB cancer cells...
  47. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits 2050, South Africa
    Nat Prod Rep 24:191-222. 2007
    ..150 references are cited...
  48. ncbi Phenanthroindolizidine alkaloids from the stems of Ficus septica
    Amooru G Damu
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, Republic of China
    J Nat Prod 68:1071-5. 2005
    ..The structures of the new compounds were elucidated by means of spectroscopic data interpretation. Cytotoxicity of some of these alkaloids was assessed in vitro using the HONE-1 and NUGC cell lines...
  49. ncbi A short route toward chiral, polyhydroxylated indolizidines and quinolizidines
    Steven H L Verhelst
    Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, P O Box 9502, 2300 RA Leiden, The Netherlands
    J Org Chem 68:9598-603. 2003
    ..Furthermore, nucleophilic substitution of the iodomethyl indolizidine as well as the aziridinium intermediate gives access to highly functionalized indolizidine and quinolizidine alkaloids...
  50. ncbi First total synthesis of phenylpyridine analogues of the antimitotic rhazinilam
    E Pasquinet
    Institut de Recherche en Chimie Organique Fine, UMR 6014, , B.P. 08, 76131 Mont Saint Aignan Cedex, France
    J Org Chem 66:2654-61. 2001
    ..Biological evaluation of compounds bearing a quaternary picolinic carbon showed interactions with tubulin similar to (-)-rhazinilam but at a lower level...
  51. ncbi Concise total synthesis of (+/-)-marcfortine B
    Barry M Trost
    Department of Chemistry, Stanford University, Stanford, California 94305 5080, USA
    J Am Chem Soc 129:3086-7. 2007
  52. pmc Total synthesis of (S)-(+)-tylophorine via enantioselective intramolecular alkene carboamination
    Wei Zeng
    Department of Chemistry, The University at Buffalo, The State University of New York, Buffalo, New York 14260, USA
    J Org Chem 73:6045-7. 2008
    ..A copper (II)-catalyzed enantioselective intramolecular alkene carboamination was employed as the key step to construct the chiral indolizidine ring...
  53. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits, South Africa
    Nat Prod Rep 25:139-65. 2008
    ..130 references are cited...
  54. ncbi Efficient synthesis of (+)-1,8,8a-tri-epi-swainsonine, (+)-1,2-di-epi-lentiginosine, (+)-9a-epi-homocastanospermine and (-)-9-deoxy-9a-epi-homocastanospermine from a D-glucose-derived aziridine carboxylate, and study of their glycosidase inhibitory activi
    K S Ajish Kumar
    Garware Research Centre, Department of Chemistry, University of Pune, Pune, 411 007, India
    Org Biomol Chem 6:703-11. 2008
    ..Glycosidase inhibitory activities of these iminosugars were investigated...
  55. ncbi Synthesis of pentahydroxy indolizidine alkaloids using ring closing metathesis: attempts to find the correct structure of uniflorine A
    Narayan S Karanjule
    Garware Research Centre, Department of Chemistry, University of Pune, Pune 411 007, India
    J Org Chem 71:6273-6. 2006
    ....
  56. ncbi Application of the palladium-catalyzed borylation/Suzuki coupling (BSC) reaction to the synthesis of biologically active biaryl lactams
    Olivier Baudoin
    Institut de Chimie des Substances Naturelles, CNRS, Avenue de la Terrasse, 91198 Gif sur Yvette, France
    J Org Chem 67:1199-207. 2002
    ..These compounds exhibit moderate albeit significant cytotoxicities and may serve as structural models for future medicinal chemistry developments...
  57. ncbi Free energy perturbation calculations on glucosidase-inhibitor complexes
    F M Ruiza
    Instituto de Física de Líquidos y Sistemas Biológicos, IFLYSIB, and Departamento de Ciencias Biológicas, Fac de Ciencias Exactas Universidad Nacional de La Plata, c c 565, B1900BTE, La Plata, Argentina
    Med Chem 1:455-60. 2005
    ..As the method uses only the crystallographic structure of the receptor, it is possible to test the possible efficiency of even still not synthesised ligands, making the pre-selection of compounds much easy and faster...
  58. ncbi Indolizidine and quinolizidine alkaloids
    Joseph P Michael
    Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Wits 2050, South Africa
    Nat Prod Rep 19:719-41. 2002
    ..tunicates and coccinellid beetles. The literature from July 2000 to June 2001 is reviewed, and 172 references are cited...
  59. ncbi Divergent cycloaddition and ring-closing metathesis approaches to indolizidine and pyrrolo[1,2-a]azepine skeletons from a chiral precursor: an expeditious route to (-)-8-epi-swainsonine triacetate
    Madhumita Nath
    Indian Institute of Chemical Biology, Kolkata
    Org Lett 8:317-20. 2006
    ....
  60. ncbi Convergent approach to pumiliotoxin alkaloids. Asymmetric total synthesis of (+)-pumiliotoxins A, B, and 225F
    Sakae Aoyagi
    School of Pharmacy, Tokyo University of Pharmacy and Life Science, Horinouchi, Hachioji, Tokyo 192 0392, Japan
    J Org Chem 67:5517-26. 2002
    ....
  61. ncbi General strategy for the construction of enantiopure pyrrolidine-based alkaloids. Total synthesis of (-)-monomorine
    Suhong Zhang
    Department of Chemistry, University of New Orleans, New Orleans, Louisiana 70148, USA
    J Org Chem 72:3133-6. 2007
    ..The synthetic utility of this compound as a chiral building block was demonstrated by a short and efficient synthesis of the pyrrolidine-based alkaloid (-)-monomorine (six steps, 37% overall yield)...
  62. ncbi Bis(oxazoline) Lewis acid catalyzed aldol reactions of pyridine N-oxide aldehydes--synthesis of optically active 2-(1-hydroxyalkyl)pyridine derivatives: development, scope, and total synthesis of an indolizine alkaloid
    Aitor Landa
    Danish National Research Foundation, Center for Catalysis, Department of Chemistry, Aarhus University, 8000 Aarhus C, Denmark
    Chemistry 12:3472-83. 2006
    ..As a synthetic application of the developed method, a full account for the asymmetric total synthesis of a nonnatural indolizine alkaloid is provided...
  63. ncbi Total synthesis of (-)-rhazinilam: asymmetric C[bond]H bond activation via the use of a chiral auxiliary
    James A Johnson
    Department of Chemistry, Columbia University, New York, New York 10027, USA
    J Am Chem Soc 124:6900-3. 2002
    ..This was achieved by the attachment of chiral platinum complexes to the proximal nitrogen atom. A high degree of selectivity (60-75% ee) was achieved via the use of oxazolinyl ketone chiral auxiliaries...
  64. ncbi A general, convergent strategy for the construction of indolizidine alkaloids: total syntheses of (-)-indolizidine 223AB and alkaloid (-)-205B
    Amos B Smith
    Department of Chemistry, Monell Chemical Senses Center and Laboratory for Research on the Structure of Matter, University of Pennsylvania, Philadelphia, PA 19104, USA
    J Org Chem 71:2547-57. 2006
    ....
  65. ncbi A versatile approach for the asymmetric syntheses of (1R,9aR)-epiquinamide and (1R,9aR)-homopumiliotoxin 223G
    Pei Qiang Huang
    Department of Chemistry and The Key Laboratory for Chemical Biology of Fujian Province, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, Fujian 361005, P R China
    Org Lett 8:1435-8. 2006
    ..An unexpected NaN(3)-promoted methanesulfonic acid elimination yielded 17, a reaction which could be useful for the syntheses of 8-dehydrodesmethylpumiliotoxins such as alkaloid 235C (3)...
  66. ncbi A concise and convergent route to 5,8-disubstituted indolizidine and 1,4-disubstituted quinolizidine ring cores by diastereoselective aza-Diels-Alder reaction
    José Barluenga
    Instituto Universitario de Quimica Organometalica Enrique Moles, Unidad Asociada al C S I C, Universidad de Oviedo, 33071 Oviedo, Spain
    Org Lett 4:1971-4. 2002
    ..The bicyclic alkaloid analogues are obtained with total diastereoselectivity and through a common pathway...
  67. doi Synthesis of rhazinicine by a metal-catalyzed C-H bond functionalization strategy
    Elizabeth M Beck
    Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
    Angew Chem Int Ed Engl 47:3004-7. 2008
  68. ncbi Design of new cognition enhancers: from computer prediction to synthesis and biological evaluation
    Athina A Geronikaki
    School of Pharmacy, Department of Pharmaceutical Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece
    J Med Chem 47:2870-6. 2004
    ..diazepines, triazepines), fused five+six-membered heterocycles (indoles, benzothiazoles, purines, indolizines, neutral, mesoionic, and cationic azolopyridines)...
  69. ncbi Assessing the superelectrophilic dimension through sigma-complexation, SNAr and Diels-Alder reactivity
    Erwin Buncel
    Department of Chemistry, Queen s University, Kingston, Ontario, Canada K7L 3N6
    Org Biomol Chem 8:2285-308. 2010
    ..Of particular interest is the synthesis of a number of indoles, indolizines, pyrroles and extended pi-excessive aromatic structures like azulene substituted by superelectrophilic moieties...
  70. ncbi Tandem [8 + 2] cycloaddition--[2 + 6 + 2] dehydrogenation reactions involving imidazo[1,2-a]pyridines and imidazo[1,2-a]pyrimidines
    Maialen Aginagalde
    Kimika Organikoa I Saila, Universidad del Pais Vasco Euskal Herriko Unibertsitatea UPV EHU, P K 1072, 20018 San Sebastián Donostia, Spain
    J Org Chem 75:2776-84. 2010
    The reaction between benzynes and imidazo[1,2-a]pyridines (pyrimidines) to form benzo[a]imidazo[5,1,2-cd]indolizines and 2,3,9c-triazocyclopenta[j,k]fluorenes has been studied computationally and experimentally...
  71. ncbi Recent developments in the combinatorial synthesis of nitrogen heterocycles using solid phase technology
    P M Chauhan
    Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, India
    Comb Chem High Throughput Screen 4:35-51. 2001
    ..describes the solid phase synthesis of azepanes, benzodiazepines, benzimidazoles, benzothiazepines, cinnolines, indolizines, beta lactams, oxazepins, oxazoles including benzisooxazoles, hydantoins, piperidines, pyrimidines, pyrazolones,..
  72. ncbi Direct palladium-catalyzed arylations of aryl bromides with 2/9-substituted pyrimido[5,4-b]indolizines
    Min Jiang
    State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203 PR China
    J Comb Chem 11:806-8. 2009
    C-5 arylated 2/9-substituted pyrimido[5,4-b]indolizines were synthesized via palladium-catalyzed direct arylation...
  73. ncbi The chemistry of [1,2,3]triazolo[1,5-a]pyridines
    Belén Abarca-González
    Departamento de Quimica Organica, Facultad de Farmacia, Universidad de Valencia, Avda Vicente Andres Estelles s n, 46100 Burjassot, Valencia, Spain
    J Enzyme Inhib Med Chem 17:359-67. 2002
    ..used, giving different types of adducts: stable disubstituted triazolopyridinium ylides of type 19 and 20, indolizines 21, or pyrroleninylpyrazolo[5,1-a] pyridines 22...
  74. pmc Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2
    Rob C Oslund
    Departments of Chemistry and Biochemistry, University of Washington, Seattle, Washington 98195, USA
    J Med Chem 51:4708-14. 2008
    ..series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor...
  75. ncbi Highly Regioselective Palladium-Catalyzed Oxidative Coupling of Indolizines and Vinylarenes via C-H Bond Cleavage
    Yuzhu Yang
    Department of Chemistry, Zhejiang University, Hangzhou 310027, People s Republic of China
    Org Lett 11:5606-9. 2009
    A highly regioselective oxidative coupling reaction between indolizines and vinylarenes has been accomplished in the presence of palladium catalysts to give only the branched alpha-product in high efficiency...
  76. ncbi Pyridine activation via copper(I)-catalyzed annulation toward indolizines
    José Barluenga
    Instituto Universitario de Quimica Organometalica Enrique Moles, Unidad Asociada al CSIC, Universidad de Oviedo, Julian Claveria 8, 33006 Oviedo, Spain
    J Am Chem Soc 132:13200-2. 2010
    ..The process represents the first successful example of metal-catalyzed cyclization of a π-deficient heterocyclic system with alkenyldiazo compounds...
  77. ncbi An efficient approach to 3,4-disubstituted pyridin-2-ones. Formal synthesis of mappicine ketone
    Ching H Lin
    Department of Chemistry, National Sun Yat Sen University, Kaohsiung, Taiwan 804, Republic of China
    J Org Chem 68:5688-91. 2003
    ..Treatment of 3,4-dihydro-3-tosylpyridin-2-one 5 with sodium hydride and then alkyl halides gave various 3,4-disubstituted pyridin-2-ones 6. Formal synthesis of mappicine ketone (1) was also reported...
  78. ncbi Synthesis of 2-azaindolizines by using an iodine-mediated oxidative desulfurization promoted cyclization of N-2-pyridylmethyl thioamides and an investigation of their photophysical properties
    Fumitoshi Shibahara
    Department of Chemistry, Faculty of Engineering, Gifu University, Yanagido, Gifu 501 1193, Japan
    Org Lett 8:5621-4. 2006
    ..The 2-azaindolizines prepared in this manner are readily converted to a variety of fluorescent compounds by using transition-metal-catalyzed cross-coupling reactions. [reaction: see text]...
  79. ncbi [Hypotensive effect of a new calcium antagonist, SR 33557 in conscious rats]
    C Lacour
    Sanofi Recherche, Montpellier, France
    Arch Mal Coeur Vaiss 83:1281-4. 1990
    ..100 at 60 mg/kg (basal values: 130 +/- 7 and 133 +/- 2 mmHg). At 30 mg/kg, the hypotension lasted for 8 hours. SR was roughly 10 times less hypotensive in WKY than in SHR. HR did not change.(ABSTRACT TRUNCATED AT 250 WORDS)..
  80. ncbi Structure of (+)-(7S,SS)-1,2,3,5,6,7-hexahydro-7-methyl-8-(p-tolylsulfinyl)-5-indoli zinone
    D H Hua
    Department of Chemistry, Kansas State University, Manhattan 66506
    Acta Crystallogr C 46:1306-8. 1990
    ..07 cm-1, F(000) = 616, T = 296 K, R = 0.049, 928 unique observed reflections. The structure determination combined with the known S configuration at the sulfur site discloses the stereochemistry of the title compound to be 7S and SS...
  81. ncbi Concise synthesis of (+/-)-rhazinilam through direct coupling
    Alfred L Bowie
    Department of Chemistry, University of California, Berkeley, California 94720, USA
    Org Lett 7:5207-9. 2005
    ..reaction: see text] A concise synthesis of rhazinilam through direct, palladium-catalyzed, intramolecular coupling is described...
  82. ncbi Encapsulation of isotope on novel beta-emitting poly(ethylene terephthalate) surfaces
    X Qu
    Department of Medicine, Interventional Cardiology Center, Columbia University, 161 Fort Washington Avenue, AP-551, New York, New York 10032, USA
    J Biomed Mater Res 57:619-23. 2001
    ..Optimal results were obtained by serially coating with two polyurethane solutions. This approach holds promise for simplifying and improving the safety, and minimizing the cost of intravascular brachytherapy...
  83. pmc Inhibition of human immunodeficiency virus syncytium formation and virus replication by castanospermine
    B D Walker
    Infectious Disease Unit, Massachusetts General Hospital, Boston
    Proc Natl Acad Sci U S A 84:8120-4. 1987
    ..The antiviral effects of castanospermine may be due to modifications of the envelope glycoprotein that affect the ability of the virus to enter cells after attachment to the CD4 cell receptor...
  84. ncbi Anti-inflammatory mechanisms of phenanthroindolizidine alkaloids
    Cheng Wei Yang
    Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Taipei, Taiwan, Republic of China
    Mol Pharmacol 69:749-58. 2006
    ..Thus, NSTP0G01 exerts its anti-inflammatory effects by inhibiting expression of the proinflammatory factors and related signaling pathways...
  85. ncbi Flueggines A and B, two new dimeric indolizidine alkaloids from Flueggea virosa
    Bing Xin Zhao
    Institute of Traditional Chinese Medicine and Natural Products, Jinan University, Guangzhou 510632, People s Republic of China
    Org Lett 13:3888-91. 2011
    ..Compound 2 exhibited growth inhibitory activity against MCF-7 and MDA-MB-231 human breast cancer cells...
  86. ncbi 9-Aryl-1,2-dihydropyrrolo[3,4-b]indolizin-3-one (Seoul-Fluor) as a smart platform for colorful ratiometric fluorescent pH sensors
    Eunha Kim
    Department of Chemistry, Seoul National University, Seoul 151 747, Korea
    Chem Commun (Camb) 47:7734-6. 2011
    ..Seoul-Fluor-based fluorescent pH sensors allow the emission- and pH-tuning ability upon protonation by varying their pK(a) values and electronic characteristics of substituents by a rational design...
  87. ncbi Evaluation of the excretion and metabolism of the new analgesic agent RWJ-22757 in male and female CR Wistar rats
    W N Wu
    Division of Preclinical Development, The R W Johnson Pharmaceutical Research Institute, Welsh and McKean Roads, Spring House, PA 19477, USA
    J Pharm Biomed Anal 28:659-71. 2002
    ....
  88. ncbi Two-component method to enantiopure quinolizidinones and Indolizidinones. Total synthesis of (-)-lasubine II
    D Ma
    State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China
    Org Lett 3:3927-9. 2001
    ..Hydrolysis of 4 to the corresponding carboxylic acids followed by treatment of acetic anhydride/triethylamine gives 3 in high yields. Using 3a as a key intermediate, (-)-lasubine II is synthesized in four steps. [reaction: see text]..
  89. ncbi Antitumor agents 251: synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents
    Linyi Wei
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem 14:6560-9. 2006
    ..16 and 0.27 microM, respectively, which are comparable to those of currently used antitumor drugs. A structure-activity relationship (SAR) study was also explored to facilitate the further development of this new compound class...
  90. ncbi Synthesis of optically active trifluoromethylated indolizidine derivatives via stereoselective radical cyclization
    Takashi Okano
    Department of Applied Chemistry, Graduate School of Engineering, Nagoya University, Furo cho, Chikusa ku, Nagoya 464 8603, Japan
    Org Lett 4:1571-3. 2002
    ..Hydrolyzed enantiomerically pure ketoacids were cyclized to dihydropyridinones. N-Iodopropylation followed by radical cyclization gave optically active trifluoromethylated indolizidinones stereoselectively...
  91. ncbi Indium-catalyzed cycloisomerizations of cyclopropene-3,3-dicarbonyl compounds: efficient access to benzo-fused heteroaromatics and heterobiaryls
    Lien H Phun
    School of Chemistry and Biochemistry, Georgia Institute of Technology, 901 Atlantic Drive, Atlanta, GA 30332 USA http www chemistry gatech edu faculty France
    Angew Chem Int Ed Engl 51:3198-202. 2012
    ..This method is amenable to a diverse array of heteroaromatics, thus allowing rapid access to benzothiophenes, benzofurans, indoles, indolizines, and pyrido[1,2-a]indoles (see scheme; Tf=trifluoromethanesulfonyl).
  92. ncbi 4,4,9,9-Tetraphenyl pyrroloindolizine: a structural analogue of calix[2]pyrrole
    K C Gowri Sreedevi
    Photosciences and Photonics Section, National Institute for Interdisciplinary Science and Technology NIIST CSIR, Trivandrum, Kerala, India
    Org Biomol Chem 10:3600-5. 2012
    ..Detailed NMR spectroscopic studies along with single crystal X-ray analysis confirm the assigned structure of the molecule...
  93. pmc Tyrosine sulfation, a post-translational modification of microvillar enzymes in the small intestinal enterocyte
    E M Danielsen
    Department of Biochemistry C, Panum Institute, University of Copenhagen, Denmark
    EMBO J 6:2891-6. 1987
    ..Most if not all the sulfate was bound to tyrosine residues rather than to the carbohydrate of the microvillar enzymes, showing that this type of modification can occur on plasma membrane proteins as well as on secretory proteins...
  94. ncbi Avermectin/milbemycin resistance in trichostrongyloid nematodes
    J H Gill
    Microbial Screening Technologies, Kemps Creek, NSW, Australia
    Int J Parasitol 28:863-77. 1998
    ..If, for different species, the critical event(s) leading to expulsion are different, then it follows that the mechanisms of resistance observed may also differ...
  95. ncbi Rhazinilam-Leuconolam-Leuconoxine Alkaloids from Leuconotis griffithii
    Chew Yan Gan
    Department of Chemistry, University of Malaya, Kuala Lumpur, Malaysia
    J Nat Prod 76:957-64. 2013
    ..Alkaloids 1, 5, and 7 showed only moderate to weak cytotoxicity toward KB cells (IC50 12-18 μg/mL), while 8 showed moderate activity in reversing MDR in vincristine-resistant KB cells...
  96. pmc Palladium-catalyzed carbonylative cyclization/arylation cascade for 2-aroylindolizine synthesis
    Zhou Li
    Department of Chemistry, University of Illinois at Chicago, 845 West Taylor Street, Chicago, Illinois 60607 7061, USA
    Org Lett 14:6056-9. 2012
    ..This transformation proceeds via the 5-endo-dig cyclization of 2-propargylpyridine triggered by an aroyl Pd complex. It produced diversely substituted 2-aroylindolizines in good to excellent yields...
  97. ncbi Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking
    Sudhanshu Kumar Bharti
    Department of Biochemistry, Patna University, Patna 800005, Bihar, India
    Phytomedicine 20:24-31. 2012
    ..The molecular docking showed that among the three alkaloids of seed extract 7-Deoxy-6-epi-castanospermine is a potent DPP-IV inhibitor similar to berberine...
  98. ncbi Calnexin and other factors that alter translocation affect the rapid binding of ubiquitin to apoB in the Sec61 complex
    Y Chen
    Molecular Medicine Unit, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, Massachusetts 02215, USA
    J Biol Chem 273:11887-94. 1998
    ..Thus, ubiquitin can be attached to unassembled apolipoprotein B in the Sec61 complex, and this process is affected by factors including calnexin that alter the translocation of apolipoprotein B...
  99. ncbi Synthesis of 1-deoxy-1-hydroxymethyl- and 1-deoxy-1-epi-hydroxymethyl castanospermine as new potential immunomodulating agents
    Vinod P Vyavahare
    Garware Research Centre, Department of Chemistry, University of Pune, Pune 411 007, India
    J Med Chem 50:5519-23. 2007
    ..The bioactivity was mediated through up-regulation of T(H1)/T(H2) cytokine ratio. The finding suggested that immunmodulatory activity of polyhydroxylated indolizidine alkaloids can be tuned by minor structural/stereochemical alterations...
  100. ncbi A novel tylophorine analog NK-007 ameliorates colitis through inhibition of innate immune response
    Ti Wen
    Department of Medical Oncology, The First Hospital of China Medical University, Shenyang 110001, China
    Int Immunopharmacol 14:487-94. 2012
    ..Moreover, Raw cells treated with NK-007 also showed decreased phosphorylation of NF-κB, which may explain the protective immune-regulatory effect of NK-007 for experimental colitis...
  101. ncbi Synthesis and evaluation of the anti-proliferative and NF-κB activities of a library of simplified tylophorine analogs
    Micah J Niphakis
    Department of Medicinal Chemistry and the Institute for Therapeutics Discovery and Development, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN 55414, USA
    Bioorg Med Chem 20:5893-900. 2012
    ..This work suggests that ring E of tylophorine is essential for the anti-proliferative activity of the 6,7,10,11-tetramethoxy-1,2,3,4-tetrahydrodibenzo[f,h]isoquinoline core scaffold...

Research Grants20

  1. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....
  2. Au/Pt Catalysis in the Synthesis of Elaborate N-Heterocycles: Methodology Develop
    Liming Zhang; Fiscal Year: 2013
    ..be designed and thus allow efficient synthesis of various N-heterocycles, including pyrrolo[2,1-a]isoindoles, indolizines, pyrrolizines, 1,2-heterocycle/carbocycle-fused indoles, pyrrolidinones, tetracyclic indolines, and ..
  3. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2013
    ..Synthetic targets for the proposed research include various diversely substituted indolizines not easily available by existing techniques, potential selective group V sPLA2 inhibitors;lamellarin D and its ..
  4. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..The photodesulfmylation of sulfinamides represents an important new protocol, not requiring acids or bases, for the removal of the valuable amine N-sulfinyl protecting group. ..
  5. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  6. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  7. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  8. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  9. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  10. Agilent 5973 GC/MS System
    GARY MOLANDER; Fiscal Year: 2002
    ..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
  11. Molecular Target Focused Discovery of Anticancer Drugs
    George R Pettit; Fiscal Year: 2010
    ....
  12. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  13. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2009
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  14. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  15. MULTIVALENT LIGANDS FOR NICOTINIC RECEPTORS
    Richard Fitch; Fiscal Year: 2007
    ..If successful, these studies will form the basis for a general approach to the three-dimensional (3D) crystallization of membrane proteins for x-ray structural analysis. [unreadable] [unreadable]..
  16. Purification of Oligonucleotides and Nucleoside Triphosphates
    William Pearson; Fiscal Year: 2007
    ..The proposed work seeks to further develop an entirely new method for oligonucleotide purification, thus streamlining the development and production of these crucial substances. [unreadable] [unreadable] [unreadable]..
  17. Catalytic Processes for Selective Organic Synthesis
    GARY MOLANDER; Fiscal Year: 2005
    ..4) Carbometalation/cyclization reactions will be explored utilizing organochromium species. 5) Ligands and catalytic systems designed for asymmetric synthesis will be explored. ..
  18. Purification of Optically Labeled Oligonucleotides
    William Pearson; Fiscal Year: 2004
    ..Initial work will focus on oligonucleotide probe purification. ..
  19. SYNTHESIS AND SYNTHETIC UTILITY OF 1-ACYLDIHYDROPYRIDINE
    DANIEL COMINS; Fiscal Year: 2004
    ..The proposed methodology will be useful for the synthesis of compounds having a broad range of biological properties, i.e. neuroleptic, antihypertensive, anti-inflammatory, anticancer, anti-AIDS, and anticonvulsant activities. ..
  20. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..