Gary Posner

Summary

Affiliation: Johns Hopkins University
Country: USA

Publications

  1. ncbi request reprint Low-calcemic vitamin D analogs (deltanoids) for human cancer prevention
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Nutr 132:3802S-3803S. 2002
  2. ncbi request reprint Mild, fast, and stereoselective epoxide opening by ketone enolate anions. Application to synthesis of the norlignan curculigine
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Org Chem 68:3049-54. 2003
  3. pmc Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Steroid Biochem Mol Biol 103:213-21. 2007
  4. ncbi request reprint Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodents
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, Maryland 21218 2685, USA
    J Med Chem 47:1299-301. 2004
  5. ncbi request reprint Low-calcemic, efficacious, 1alpha,25-dihydroxyvitamin D3 analog QW-1624F2-2: calcemic dose-response determination, preclinical genotoxicity testing, and revision of A-ring stereochemistry
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, USA
    Steroids 69:757-62. 2004
  6. ncbi request reprint Knowledge of the proposed chemical mechanism of action and cytochrome p450 metabolism of antimalarial trioxanes like artemisinin allows rational design of new antimalarial peroxides
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Acc Chem Res 37:397-404. 2004
  7. ncbi request reprint Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1alpha,25-dihydroxyvitamin D3
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218 2685, USA
    J Steroid Biochem Mol Biol 89:5-12. 2004
  8. ncbi request reprint Malaria-infected mice are cured by a single dose of novel artemisinin derivatives
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins Malaria Research Institute, Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Med Chem 50:2516-9. 2007
  9. ncbi request reprint Novel A-ring analogs of the hormone 1alpha,25-dihydroxyvitamin D3: synthesis and preliminary biological evaluation
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 13:2959-66. 2005
  10. ncbi request reprint Highly antiproliferative, low-calcemic, side-chain ketone analogs of the hormone 1alpha,25-dihydroxyvitamin D3
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 13:5569-80. 2005

Research Grants

Collaborators

Detail Information

Publications55

  1. ncbi request reprint Low-calcemic vitamin D analogs (deltanoids) for human cancer prevention
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Nutr 132:3802S-3803S. 2002
    ..A short summary is provided of leading chemopreventive analogs of vitamin D3...
  2. ncbi request reprint Mild, fast, and stereoselective epoxide opening by ketone enolate anions. Application to synthesis of the norlignan curculigine
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Org Chem 68:3049-54. 2003
    ....
  3. pmc Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Steroid Biochem Mol Biol 103:213-21. 2007
    ..The transcriptional activity of the 25-CHF(2) analog 3 is higher than that of the 1-CHF(2) analog 4...
  4. ncbi request reprint Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodents
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, Maryland 21218 2685, USA
    J Med Chem 47:1299-301. 2004
    ..In the transgenic adenocarcinoma of mouse prostate model, some of the trioxane dimers had potent anticancer activity...
  5. ncbi request reprint Low-calcemic, efficacious, 1alpha,25-dihydroxyvitamin D3 analog QW-1624F2-2: calcemic dose-response determination, preclinical genotoxicity testing, and revision of A-ring stereochemistry
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, USA
    Steroids 69:757-62. 2004
    ..This analog is shown to be approximately 80-100 times less calciuric than the natural hormone 1alpha,25-dihydoxyvitamin D3. This analog is shown also to be non-genotoxic in three different standard assays...
  6. ncbi request reprint Knowledge of the proposed chemical mechanism of action and cytochrome p450 metabolism of antimalarial trioxanes like artemisinin allows rational design of new antimalarial peroxides
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Acc Chem Res 37:397-404. 2004
    ..Incorporating metabolism-blocking substituents also provides some new, potent, semi-synthetic artemisinin derivatives...
  7. ncbi request reprint Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1alpha,25-dihydroxyvitamin D3
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218 2685, USA
    J Steroid Biochem Mol Biol 89:5-12. 2004
    ..The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1alpha,25-dihydroxyvitamin D(3), is a potent (IC(50) = 28nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24...
  8. ncbi request reprint Malaria-infected mice are cured by a single dose of novel artemisinin derivatives
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins Malaria Research Institute, Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Med Chem 50:2516-9. 2007
    ..Four of these trioxane dimers cure malaria-infected mice after only a single subcutaneous dose, and two other dimers cure after three oral doses...
  9. ncbi request reprint Novel A-ring analogs of the hormone 1alpha,25-dihydroxyvitamin D3: synthesis and preliminary biological evaluation
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 13:2959-66. 2005
    ....
  10. ncbi request reprint Highly antiproliferative, low-calcemic, side-chain ketone analogs of the hormone 1alpha,25-dihydroxyvitamin D3
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 13:5569-80. 2005
    ..In addition, ketone analog 19-nor-2a is not significantly less calcemic in vivo than 19-methylene analog 2a...
  11. ncbi request reprint Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
    J Med Chem 46:1060-5. 2003
    ....
  12. ncbi request reprint A non-calcemic sulfone version of the vitamin D(3) analogue seocalcitol (EB 1089): chemical synthesis, biological evaluation and potency enhancement of the anticancer drug adriamycin
    G H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 9:2365-71. 2001
    ..8 cells, binds poorly but measurably to the vitamin D receptor (VDR), and desirably is non-calcemic in vivo at a daily dose (7 days) of 10 microg/kg of rat body weight...
  13. ncbi request reprint Conceptually new 20-epi-22-oxa sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and biological evaluation
    G H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Med Chem 43:3581-6. 2000
    ..s KH-1060 (3), is recognized by catabolic enzymes, the selective biological profile of sulfone 4a is likely not due to its metabolites that are formed in only minor amounts...
  14. doi request reprint Malaria-infected mice are cured by oral administration of new artemisinin derivatives
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
    J Med Chem 51:1035-42. 2008
    ..7-13.7, and this effect is comparable to that of the fully synthetic trioxolane drug development candidate OZ277, which is in phase II clinical trials...
  15. ncbi request reprint Conceptually new low-calcemic oxime analogues of the hormone 1 alpha,25-dihydroxyvitamin D(3): synthesis and biological testing
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Med Chem 45:1723-30. 2002
    ..In terms of in vivo toxicity (hypercalcemia), ketone 2b is strongly calcemic in rats, whereas oxime 3b and oxime ether 4b are considerably less calcemic (i.e., safer) than calcitriol (1)...
  16. pmc Electronically stabilized versions of the antimalarial acetal trioxanes artemether and artesunate
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218, USA
    Bioorg Med Chem 16:5247-53. 2008
    ..The very strong inductive electron-withdrawing C-9 substituent is shown to retard considerably C-10 ionization (acid-promoted etherification) of 9-fluoro-DHA and 9-sulfonyl-DHA...
  17. ncbi request reprint Conceptually new deltanoids (vitamin D analogs) inhibit multistage skin tumorigenesis
    T W Kensler
    Department of Environmental Health Sciences and Department of Epidemiology, School of Hygiene and Public Health, The Johns Hopkins University, Baltimore, MD 21205, USA
    Carcinogenesis 21:1341-5. 2000
    ....
  18. ncbi request reprint Conformationally restricted hybrid analogues of the hormone 1 alpha,25-dihydroxyvitamin D(3): design, synthesis, and biological evaluation
    M C White
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 9:1691-9. 2001
    ....
  19. ncbi request reprint Metabolites and analogs of 1alpha,25-dihydroxyvitamin D(3): evaluation of actions in bone
    S Kadiyala
    Osiris Therapeutics, Baltimore, MD, USA
    Steroids 66:347-55. 2001
    ..On the other hand, while the C-1alpha-hydroxyl group is necessary for activation of genomic events via nVDR, the activation of nongenomic events occurs in the absence of this group...
  20. ncbi request reprint Vitamin D analogs as anti-carcinogenic agents
    E S Agoston
    Department of Pharmacology and Molecular Sciences, School of Medicine, Johns Hopkins University, Baltimore, MD 21205, USA
    Anticancer Agents Med Chem 6:53-71. 2006
    ..Lastly, there is evidence that deltanoids can enhance the activity of other chemopreventive agents. The use of a cocktail approach will be discussed as a potential avenue for deltanoids in chemoprevention and chemotherapy...
  21. ncbi request reprint Antimalarial simplified 3-aryltrioxanes: synthesis and preclinical efficacy/toxicity testing in rodents
    G H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Med Chem 44:3054-8. 2001
    ..Preclinical evaluation of this water-soluble synthetic trioxane 8a in rodents shows it to have at least as good a therapeutic index (efficacy/toxicity) as that of water-soluble semisynthetic trioxane artelinic acid (5)...
  22. ncbi request reprint Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activity
    Ik Hyeon Paik
    Department of Chemistry, The Johns Hopkins University, Baltimore, Maryland 21218 2685, USA
    J Med Chem 49:2731-4. 2006
    ....
  23. ncbi request reprint Less calcemic Vitamin D analogs enhance creatine kinase specific activity and modulate responsiveness to gonadal steroids in the vasculature
    Dalia Somjen
    Institute of Endocrinology, Metabolism and Hypertension, Tel Aviv Sourasky Medical Center, Tel Aviv, Israel
    J Steroid Biochem Mol Biol 101:232-8. 2006
    ..These results corroborate our previous in vitro studies in human vascular cells and further suggest that the Vitamin D system plays an important physiological role in maintaining normal cell energy reservoir in the vasculature...
  24. pmc In vitro inhibition of Toxoplasma gondii by four new derivatives of artemisinin
    Lorraine Jones-Brando
    Stanley Division of Developmental Neurovirology, Dept of Pediatrics, Johns Hopkins University School of Medicine, 600 N Wolfe St, Baltimore, MD 21287 4988, USA
    Antimicrob Agents Chemother 50:4206-8. 2006
    ..We synthesized novel, nonacetal, hydrolytically stable derivatives of artemisinin and showed that they inhibit the replication of Toxoplasma gondii in cell culture...
  25. ncbi request reprint Highly antiproliferative, low-calcemic, side-chain amide and hydroxamate analogs of the hormone 1alpha,25-dihydroxyvitamin D3
    Sandra Sinishtaj
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 14:6341-8. 2006
    ..Even though lacking the 25-OH group characteristic of natural calcitriol (1), analogs 2-4 are as antiproliferative in vitro as calcitriol (1) but are 20-40 times less calciuric in vivo than calcitriol (1)...
  26. ncbi request reprint QW-1624F2-2, a synthetic analogue of 1,25-dihydroxyvitamin D3, enhances the response to other deltanoids and suppresses the invasiveness of human metastatic breast tumor cells
    Sujatha Sundaram
    Department of Surgery, Dartmouth Medical School, One Medical Center Drive, HB 7850, Lebanon, NH 03756, USA
    Mol Cancer Ther 5:2806-14. 2006
    ..QW also blocked the sustained induction of CYP24 expression by 1,25(OH)(2)D(3) and EB 1089, increased the potency of 1,25(OH)(2)D(3) and EB 1089, and inhibited breast tumor cell proliferation and invasion...
  27. pmc Differentiation-inducing potency of the seco-steroid JK-1624F2-2 can be increased by combination with an antioxidant and a p38MAPK inhibitor which upregulates the JNK pathway
    Jing Zhang
    Department of Pathology and Laboratory Medicine, UMDNJ New Jersey Medical School, Newark, NJ 07103, USA
    J Steroid Biochem Mol Biol 105:140-9. 2007
    ..Further, since JKF is less calcemic than 1,25D, the data suggest that JKF combined with CA and SB is likely to have a therapeutic advantage over 1,25D-based experimental regimens for myeloid leukemias...
  28. ncbi request reprint Biological mechanisms of action of novel C-10 non-acetal trioxane dimers in prostate cancer cell lines
    Adebusola A Alagbala
    Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    J Med Chem 49:7836-42. 2006
    ..TDs also promoted apoptosis in LNCaP cells with increased expression of proapoptotic bax. These results demonstrate that TDs are potentially useful agents that warrant further preclinical development for treatment of prostate cancer...
  29. ncbi request reprint A 24-phenylsulfone analog of vitamin D inhibits 1alpha,25-dihydroxyvitamin D(3) degradation in vitamin D metabolism-competent cells
    Daniel Lechner
    Department of Pathophysiology, Medical University of Vienna, Waehringer Guertel 18 20, A 1090 Vienna, Austria
    J Pharmacol Exp Ther 320:1119-26. 2007
    ..Yet, S-4a imparts antimitotic activity to 1alpha,25-(OH)(2)D(3) and may therefore constitute a therapeutic to stimulate the antiproliferative potential of vitamin D-based antitumor activity...
  30. ncbi request reprint Antitumor effects of two less-calcemic vitamin D analogs (Paricalcitol and QW-1624F2-2) in squamous cell carcinoma cells
    Adebusola A Alagbala
    Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Buffalo, N Y, USA
    Oncology 70:483-92. 2006
    ..These less-calcemic vitamin D analogs are as effective as calcitriol in vitro and are promising for prevention and treatment of cancer and other diseases...
  31. ncbi request reprint Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation
    Sara Peleg
    Department of Endocrine Neoplasia and Hormonal Disorders, The University of Texas, M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Med Chem 49:7513-7. 2006
    ..Both of these two hybrid analogs are as transcriptionally active as calcitriol and are strongly antiproliferative in vitro but are low-calcemic in vivo...
  32. ncbi request reprint Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation
    Kimberly S Petersen
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Med Chem 50:5824-32. 2007
    ..One of these three 23-oxa analogs has transcriptional potency almost as high as that of calcitriol, even though it binds to the human vitamin D receptor only about 1% as well as calcitriol...
  33. pmc Antiproliferative, low-calcemic, fluorinated sulfone analogs of 1alpha,25-dihydroxyvitamin D3: chemical synthesis and biological evaluation
    Aimee R Usera
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 15:5509-18. 2007
    ..Incorporation of additional fluorines, as in a perfluorobutyl analog, results in a loss of antiproliferative activity...
  34. ncbi request reprint Enantiomeric 1,2,4-trioxanes display equivalent in vitro antimalarial activity versus Plasmodium falciparum malaria parasites: implications for the molecular mechanism of action of the artemisinins
    Paul M O'Neill
    Department of Chemistry, University of Liverpool, The Robert Robinson Laboratories, Oxford Street, Liverpool, L69 7ZD, UK
    Chembiochem 6:2048-54. 2005
    ..In five different P. falciparum isolates, however, the trioxane enantiomers (+)-7 a, (-)-7 a and (+)-7 b, (-)-7 b, showed the same level of in vitro antiparasitic activity...
  35. ncbi request reprint Anticancer effects of the novel 1alpha, 25-dihydroxyvitamin D3 hybrid analog QW1624F2-2 in human neuroblastoma
    C Damodar Reddy
    Division of Neurosurgery, The Children s Hospital of Philadelphia and The Abramson Family Cancer Research Institute, Philadelphia, PA 19104, USA
    J Cell Biochem 97:198-206. 2006
    ..In summary, the low-calcemic hybrid analog QW showed significant anti-tumor activity in vivo and thus exhibits potential as a novel cancer therapeutic...
  36. ncbi request reprint Vitamin D analogs as modulators of vitamin D receptor action
    Sara Peleg
    Department of Endocrine Neoplasia and Hormonal Disorders, Box 435, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    Curr Top Med Chem 3:1555-72. 2003
    ..Finally, we will describe the current and potential use of these selective modulators of the VDR for treatment of human diseases such as osteoporosis, cancer, and secondary hyperparathyroidism...
  37. ncbi request reprint Vitamin D and vitamin D analogs as cancer chemopreventive agents
    Kathryn Z Guyton
    CCS Associates, 2005 Landings Drive, Mountain View, CA 94043, USA
    Nutr Rev 61:227-38. 2003
    ..The vitamin D receptor, a steroid/thyroid receptor superfamily member, appears to control most deltanoid effects on proliferation, apoptosis, differentiation, and angiogenesis...
  38. ncbi request reprint A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides
    Mario D Bachi
    Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot 76100, Israel
    J Med Chem 46:2516-33. 2003
    ..NS. In view of the nontoxicity of beta-sulfonyl peroxides 39a, 46a, and 46b in mice, at high dosing, these compounds are regarded as promising antimalarial drug candidates...
  39. ncbi request reprint New chemical and biological aspects of artemisinin-derived trioxane dimers
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 10:227-32. 2002
    ..Each dimer was evaluated in vitro for antimalarial, antiproliferative, and antitumor activities; ketone dimers and, more than fluorinated dimers and, are promising for chemotherapy of both malaria and cancer...
  40. ncbi request reprint Antimalarial chemotherapeutic peroxides: artemisinin, yingzhaosu A and related compounds
    Kristina Borstnik
    Department of Chemistry, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218 2685, USA
    Int J Parasitol 32:1661-7. 2002
    ..This review summarises recent achievements in this area of peroxide drug development for malaria chemotherapy...
  41. ncbi request reprint Malaria: new chemotherapeutic peroxide drugs
    Kristina Borstnik
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Mini Rev Med Chem 2:573-83. 2002
    ..This review summarizes recent achievements in this area of peroxide drug development for malaria chemotherapy...
  42. ncbi request reprint Orally active, water-soluble antimalarial 3-aryltrioxanes: short synthesis and preclinical efficacy testing in rodents
    Gary H Posner
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, Maryland 21218 2685, USA
    J Med Chem 45:3824-8. 2002
    ..4 than is artelinic acid (1), a leading semisynthetic, herb-derived antimalarial trioxane drug candidate...
  43. ncbi request reprint 2,2-Disubstituted analogues of the natural hormone 1 alpha,25-dihydroxyvitamin D(3): chemistry and biology
    Gary H Posner
    Department of Chemistry, Krieger School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 10:2353-65. 2002
    ..Dimethylated analogue strongly suppresses parathyroid hormone (PTH) secretion...
  44. ncbi request reprint Antimalarial and antitumor evaluation of novel C-10 non-acetal dimers of 10beta-(2-hydroxyethyl)deoxoartemisinin
    J Prince Jeyadevan
    Department of Chemistry, The Robert Robinson Laboratories, University of Liverpool, Liverpool L69 7ZD, UK
    J Med Chem 47:1290-8. 2004
    ..This observation emphasizes the importance of two trioxane units for high antiproliferative activity, and we propose that the nature of the linker in dimers of this type plays a crucial role in imparting potent anticancer activity...
  45. ncbi request reprint A medicinal chemistry perspective on artemisinin and related endoperoxides
    Paul M O'Neill
    Department of Chemistry, The Robert Robinson Laboratories, University of Liverpool, Liverpool L69 7ZD, U K
    J Med Chem 47:2945-64. 2004
  46. ncbi request reprint Inhibition of prostate cancer-meditated osteoblastic bone lesions by the low-calcemic analog 1alpha-hydroxymethyl-16-ene-26,27-bishomo-25-hydroxy vitamin D3
    Sara Peleg
    Department of Endocrine Neoplasia and Hormonal Disorders, Unit 435, The University of Texas, M D Anderson Cancer Center, Houston, TX 77030, USA
    J Steroid Biochem Mol Biol 97:203-11. 2005
    ..These experiments led to the hypothesis that, in vivo, JK-1626-2 prevented the metastatic bone lesions by inhibiting the mitogenic response of osteoblasts to growth factors produced by MDA-PCa 2b cells...
  47. ncbi request reprint A-ring hydroxymethyl 19-nor analogs of the natural hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and preliminary biological evaluation
    Mark A Hatcher
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    Bioorg Med Chem 13:3964-76. 2005
    ....
  48. ncbi request reprint Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3)
    Mehmet Kahraman
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Med Chem 47:6854-63. 2004
    ..4 nM) having low calcemic activity. In addition, this compound shows high selectivity toward the CYP24 enzyme in comparison to CYP27A1 (IC(50) > 1000 nM) and CYP27B (IC(50) = 554 nM)...
  49. ncbi request reprint Responsiveness to phytoestrogens in primary human osteoblasts is modulated differentially by a "less-calcemic" analog of 1,25 dihydroxyvitamin D(3): JK 1624F(2)-2 (JKF)
    Dalia Somjen
    Institute of Endocrinology, Metabolism and Hypertension, Tel Aviv Sourasky Medical Center, 6 Weizman St, Tel Aviv 64239, Israel
    J Steroid Biochem Mol Biol 98:139-46. 2006
    ..This study raises the possibility of combined Vitamin D analog and phytoestrogen for hormonal replacement therapy to prevent post-menopausal osteoporosis, which is a subject of ongoing research in animal models...
  50. ncbi request reprint Treatment with non-hypercalcemic analogs of 1,25-dihydroxyvitamin D3 increases responsiveness to 17beta-estradiol, dihydrotestosterone or raloxifene in primary human osteoblasts
    Sara Katzburg
    Institute of Endocrinology, Sourasky Medical Center, 6 Weizman St Tel Aviv 64239, Israel
    J Steroid Biochem Mol Biol 88:213-9. 2004
    ..This study raises the possibility of testing combined Vitamin D analog and estrogen replacement treatment for post-menopausal women to prevent osteoporosis...
  51. ncbi request reprint Estrogenic activity of glabridin and glabrene from licorice roots on human osteoblasts and prepubertal rat skeletal tissues
    Dalia Somjen
    Institute of Endocrinology, Metabolism and Hypertension, Tel Aviv Sourasky Medical Center and Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv 64239, Israel
    J Steroid Biochem Mol Biol 91:241-6. 2004
    ..Glabrene activity was not inhibited by raloxifene. Therefore, glabridin shows greater similarity to estradiol-17beta and thus greater potential, with or without Vitamin D, to modulate bone disorders in post-menopausal women...
  52. ncbi request reprint Unexpected steric effects of "remote" alkyl groups on the rate of conjugate additions to alkyl alpha,beta-ethylenic sulfones, sulfoxides, and esters
    Aimee R Usera
    Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, Maryland 21218, USA
    J Org Chem 72:2329-34. 2007
    ..Competition experiments establish the relative rates of Michael additions to be in the following order: Et>i-Pr>t-Bu...
  53. ncbi request reprint A non-calcemic Vitamin D analog modulates both nuclear and putative membranal estrogen receptors in cultured human vascular smooth muscle cells
    Dalia Somjen
    Institute of Endocrinology, Metabolism and Hypertension, Tel Aviv Sourasky Medical Center, 6 Weizman Street, Tel Aviv 64239, Israel
    J Steroid Biochem Mol Biol 89:397-9. 2004
    ..The results provide evidence that the effects of JKF on ERalpha/ERbeta as well as on membranal versus nuclear binding of estrogen are divergent and show differential modulation...
  54. ncbi request reprint Modulation of the response to estradiol-17beta of rat vascular tissues by a non calcemic vitamin D analog
    Dalia Somjen
    Tel Aviv Sourasky Medical Center, Institute of Endocrinology, Metabolism and Hypertension, 6 Weizman St, Tel Aviv 64239, Israel
    J Steroid Biochem Mol Biol 89:339-41. 2004
    ..These results should prompt examination of the possibility that the effects estrogen therapy in postmenopausal women can be augmented by vitamin D or its analogs...
  55. pmc Effect of artemisinins and other endoperoxides on nitric oxide-related signaling pathway in RAW 264.7 mouse macrophage cells
    V Badireenath Konkimalla
    German Cancer Research Center, Pharmaceutical Biology C015, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
    Nitric Oxide 19:184-91. 2008
    ..In addition, other signaling pathways also contribute to the inhibitory effect of artesunate towards RAW 264.7 cells pointing to a multi-factorial mode of action of artesunate...

Research Grants20

  1. TRIOXANES FOR CHEMOTHERAPY OF MALARIA AND CANCER
    Gary Posner; Fiscal Year: 2005
    ....
  2. Chemoprevention/Therapy Using Non-Calcemic Vitamin D
    Gary Posner; Fiscal Year: 2006
    ..Collectively, these studies will provide important structure- activity insights into the cancer chemoprotective and chemotherapeutic actions and molecular biology of vitamin D3 analogs. ..
  3. Peroxides for Chemotherapy of Malaria and Cancer
    Gary Posner; Fiscal Year: 2007
    ....
  4. MALARIA CHEMOTHERAPY AND CHEMOPROTECTION
    Gary Posner; Fiscal Year: 2000
    ....