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Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Thompson SK, Washburn DG, Frazee JS, Madauss KP, Hoang TH, Lapinski L, Grygielko ET, Glace LE, Trizna W, Williams SP, Duraiswami C, Bray JD, Laping NJ. Thompson SK, et al. Among authors: laping nj. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4777-80. doi: 10.1016/j.bmcl.2009.06.055. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19595590
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.
Hammond M, Washburn DG, Hoang HT, Manns S, Frazee JS, Nakamura H, Patterson JR, Trizna W, Wu C, Azzarano LM, Nagilla R, Nord M, Trejo R, Head MS, Zhao B, Smallwood AM, Hightower K, Laping NJ, Schnackenberg CG, Thompson SK. Hammond M, et al. Among authors: laping nj. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4441-5. doi: 10.1016/j.bmcl.2009.05.051. Epub 2009 May 18. Bioorg Med Chem Lett. 2009. PMID: 19497745
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.
Kallander LS, Washburn DG, Hoang TH, Frazee JS, Stoy P, Johnson L, Lu Q, Hammond M, Barton LS, Patterson JR, Azzarano LM, Nagilla R, Madauss KP, Williams SP, Stewart EL, Duraiswami C, Grygielko ET, Xu X, Laping NJ, Bray JD, Thompson SK. Kallander LS, et al. Among authors: laping nj. Bioorg Med Chem Lett. 2010 Jan 1;20(1):371-4. doi: 10.1016/j.bmcl.2009.10.092. Epub 2009 Oct 25. Bioorg Med Chem Lett. 2010. PMID: 19926282
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S. Gellibert F, et al. Among authors: laping nj. J Med Chem. 2006 Apr 6;49(7):2210-21. doi: 10.1021/jm0509905. J Med Chem. 2006. PMID: 16570917
85 results