George F Allan

Summary

Affiliation: Johnson and Johnson Pharmaceutical Research and Development
Country: USA

Publications

  1. ncbi Molecular properties and preclinical pharmacology of JNJ-1250132, a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro
    George F Allan
    Department of Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, 1000 US Route, 202 South, P O Box 300, Raritan, NJ 08869, USA
    Steroids 71:578-84. 2006
  2. ncbi A selective androgen receptor modulator with minimal prostate hypertrophic activity restores lean body mass in aged orchidectomized male rats
    George Allan
    Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, L L C, 1000 U S Route 202 South, Raritan, NJ, USA
    J Steroid Biochem Mol Biol 110:207-13. 2008
  3. ncbi A selective androgen receptor modulator with minimal prostate hypertrophic activity enhances lean body mass in male rats and stimulates sexual behavior in female rats
    George F Allan
    Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ, 08869, USA
    Endocrine 32:41-51. 2007
  4. ncbi Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    J Med Chem 50:3857-69. 2007
  5. ncbi 2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:955-8. 2007
  6. ncbi Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:439-43. 2007
  7. ncbi Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:1784-7. 2007
  8. ncbi Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:784-8. 2007
  9. ncbi Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 16:5763-6. 2006
  10. ncbi A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
    James C Lanter
    Johnson and Johnson Pharmaceutical Research and Development L L C, 1000 Route 202 S, Raritan, NJ 08869, USA
    Bioorg Med Chem Lett 16:5646-9. 2006

Collaborators

Detail Information

Publications14

  1. ncbi Molecular properties and preclinical pharmacology of JNJ-1250132, a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro
    George F Allan
    Department of Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, 1000 US Route, 202 South, P O Box 300, Raritan, NJ 08869, USA
    Steroids 71:578-84. 2006
    ..Therefore, JNJ-1250132 has unique effects on the progesterone receptor that may translate into a novel clinical profile...
  2. ncbi A selective androgen receptor modulator with minimal prostate hypertrophic activity restores lean body mass in aged orchidectomized male rats
    George Allan
    Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, L L C, 1000 U S Route 202 South, Raritan, NJ, USA
    J Steroid Biochem Mol Biol 110:207-13. 2008
    ..JNJ-37654032 reduced follicle-stimulating hormone levels in orchidectomized rats and reduced testis size in intact rats. JNJ-37654032 is a potent prostate-sparing SARM with the potential for clinical benefit in muscle-wasting diseases...
  3. ncbi A selective androgen receptor modulator with minimal prostate hypertrophic activity enhances lean body mass in male rats and stimulates sexual behavior in female rats
    George F Allan
    Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ, 08869, USA
    Endocrine 32:41-51. 2007
    ..JNJ-28330835 is a prostate-sparing SARM with the potential for clinically beneficial effects in muscle-wasting diseases and sexual function disorders...
  4. ncbi Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    J Med Chem 50:3857-69. 2007
    ..Thus, (S)-7c is a tissue-selective nonsteroidal androgen receptor modulator with agonist activity on muscle and mixed agonist and antagonist activity on prostate...
  5. ncbi 2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:955-8. 2007
    ..SAR studies led to the discovery of 4-bromo-benzyl benzimidazole 17 as a more potent androgen receptor antagonist in the rat prostate (ID(50)=0.13mg/day), compared with bicalutamide (ID(50)=0.23mg/day)...
  6. ncbi Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:439-43. 2007
    ..A novel imidazolopyrazole derivative has been fortuitously discovered as potent selective androgen receptor modulator with in vivo efficacy...
  7. ncbi Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:1784-7. 2007
    ..03-0.11 mg/day). True SARMs showing both prostate antagonism and levator ani agonism were revealed...
  8. ncbi Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives
    Raymond A Ng
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:784-8. 2007
    ..During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist activity in the prostate. Benzimidazole 1 is a potent AR antagonist in the rat prostate (ID50 = 0.15 mg/day)...
  9. ncbi Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 16:5763-6. 2006
    ..A novel series of hydantoin derivatives were identified by in vivo studies as tissue selective androgen receptor modulators. SAR around this series revealed that the function of the ligand could be altered by minor structural modification...
  10. ncbi A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
    James C Lanter
    Johnson and Johnson Pharmaceutical Research and Development L L C, 1000 Route 202 S, Raritan, NJ 08869, USA
    Bioorg Med Chem Lett 16:5646-9. 2006
    ..Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain...
  11. ncbi Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands
    Xuqing Zhang
    Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA
    Bioorg Med Chem Lett 16:3233-7. 2006
    ..Studies of structure-activity relationships (SARs) were investigated, which led to some compounds in this series as strong binders to androgen receptors...
  12. ncbi The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening
    James C Lanter
    Johnson and Johnson Pharmaceutical Research and Development L L C, 666 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:123-6. 2007
    ..Through the use of this paradigm, we were able to identify compounds that exhibited in vivo potency equal to that of the marketed antiandrogen Casodex when orally administered...
  13. ncbi beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model
    James C Lanter
    Johnson and Johnson Pharmaceutical Research and Development L L C, 665 Stockton Drive, Exton, PA 19341, USA
    Bioorg Med Chem Lett 17:2545-8. 2007
    ..Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model...
  14. ncbi Cell type-specific bidirectional regulation of the glucocorticoid-induced leucine zipper (GILZ) gene by estrogen
    Sharon H Tynan
    Reproductive Therapeutics, Johnson and Johnson Pharmaceutical Research and Development, L.L.C, 1000 Route 202 South, Room B-115, P.O. Box 300, Raritan, NJ 08869, USA
    J Steroid Biochem Mol Biol 91:225-39. 2004
    ..Elimination of the CREB binding site blocks both basal activity and estrogen regulation. Our results suggest that ER action at the CRE may mediate estrogen-dependent, cell-specific regulation of this gene...