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Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE. Fensome A, et al. Among authors: winneker rc. J Med Chem. 2008 Mar 27;51(6):1861-73. doi: 10.1021/jm701080t. Epub 2008 Mar 5. J Med Chem. 2008. PMID: 18318463
Novel pyrrole-containing progesterone receptor modulators.
Collins MA, Hudak V, Bender R, Fensome A, Zhang P, Miller L, Winneker RC, Zhang Z, Zhu Y, Cohen J, Unwalla RJ, Wrobel J. Collins MA, et al. Among authors: winneker rc. Bioorg Med Chem Lett. 2004 May 3;14(9):2185-9. doi: 10.1016/j.bmcl.2004.02.054. Bioorg Med Chem Lett. 2004. PMID: 15081005
Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget.
Zhang Z, Olland AM, Zhu Y, Cohen J, Berrodin T, Chippari S, Appavu C, Li S, Wilhem J, Chopra R, Fensome A, Zhang P, Wrobel J, Unwalla RJ, Lyttle CR, Winneker RC. Zhang Z, et al. Among authors: winneker rc. J Biol Chem. 2005 Aug 5;280(31):28468-75. doi: 10.1074/jbc.M504144200. Epub 2005 Jun 3. J Biol Chem. 2005. PMID: 15937332 Free article.
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Fensome A, Bender R, Chopra R, Cohen J, Collins MA, Hudak V, Malakian K, Lockhead S, Olland A, Svenson K, Terefenko EA, Unwalla RJ, Wilhelm JM, Wolfrom S, Zhu Y, Zhang Z, Zhang P, Winneker RC, Wrobel J. Fensome A, et al. Among authors: winneker rc. J Med Chem. 2005 Aug 11;48(16):5092-5. doi: 10.1021/jm050358b. J Med Chem. 2005. PMID: 16078826
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z. Zhang P, et al. Among authors: winneker rc. Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. doi: 10.1016/j.bmc.2007.07.011. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17681796
A new generation of progesterone receptor modulators.
Winneker RC, Fensome A, Zhang P, Yudt MR, McComas CC, Unwalla RJ. Winneker RC, et al. Steroids. 2008 Aug;73(7):689-701. doi: 10.1016/j.steroids.2008.03.005. Epub 2008 Mar 28. Steroids. 2008. PMID: 18472121 Review.
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