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Page 1
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J. Hamann LG, et al. Among authors: golla r. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. doi: 10.1016/j.bmcl.2007.01.076. Epub 2007 Jan 27. Bioorg Med Chem Lett. 2007. PMID: 17292608
Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.
Ostrowski J, Kuhns JE, Lupisella JA, Manfredi MC, Beehler BC, Krystek SR Jr, Bi Y, Sun C, Seethala R, Golla R, Sleph PG, Fura A, An Y, Kish KF, Sack JS, Mookhtiar KA, Grover GJ, Hamann LG. Ostrowski J, et al. Among authors: golla r. Endocrinology. 2007 Jan;148(1):4-12. doi: 10.1210/en.2006-0843. Epub 2006 Sep 28. Endocrinology. 2007. PMID: 17008401
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG. Sun C, et al. Among authors: golla r. J Med Chem. 2006 Dec 28;49(26):7596-9. doi: 10.1021/jm061101w. J Med Chem. 2006. PMID: 17181141
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.
Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR Jr, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG. Li JJ, et al. Among authors: golla r. J Med Chem. 2007 Jun 28;50(13):3015-25. doi: 10.1021/jm070312d. Epub 2007 Jun 7. J Med Chem. 2007. PMID: 17552509
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Manfredi MC, Bi Y, Nirschl AA, Sutton JC, Seethala R, Golla R, Beehler BC, Sleph PG, Grover GJ, Ostrowski J, Hamann LG. Manfredi MC, et al. Among authors: golla r. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4487-90. doi: 10.1016/j.bmcl.2007.06.007. Epub 2007 Jun 6. Bioorg Med Chem Lett. 2007. PMID: 17574413
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Wang H, Ruan Z, Li JJ, Simpkins LM, Smirk RA, Wu SC, Hutchins RD, Nirschl DS, Van Kirk K, Cooper CB, Sutton JC, Ma Z, Golla R, Seethala R, Salyan ME, Nayeem A, Krystek SR Jr, Sheriff S, Camac DM, Morin PE, Carpenter B, Robl JA, Zahler R, Gordon DA, Hamann LG. Wang H, et al. Among authors: golla r. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3168-72. doi: 10.1016/j.bmcl.2008.04.069. Epub 2008 May 1. Bioorg Med Chem Lett. 2008. PMID: 18485702
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Nirschl AA, Zou Y, Krystek SR Jr, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG. Nirschl AA, et al. Among authors: golla r. J Med Chem. 2009 May 14;52(9):2794-8. doi: 10.1021/jm801583j. J Med Chem. 2009. PMID: 19351168
85 results