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Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors.
Ramurthy S, Pfister KB, Boyce RS, Brown SP, Costales AQ, Desai MC, Fang E, Levine BH, Ng SC, Nuss JM, Ring DB, Shafer CM, Shu W, Subramanian S, Wagman AS, Wang H, Bussiere DE. Ramurthy S, et al. Among authors: brown sp. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126930. doi: 10.1016/j.bmcl.2019.126930. Epub 2019 Dec 23. Bioorg Med Chem Lett. 2020. PMID: 31926786
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.
Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE. Wagman AS, et al. Among authors: brown sp. J Med Chem. 2017 Oct 26;60(20):8482-8514. doi: 10.1021/acs.jmedchem.7b00922. Epub 2017 Oct 10. J Med Chem. 2017. PMID: 29016121
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC. Wang Y, et al. Among authors: brown sp. ACS Med Chem Lett. 2013 May 7;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900707 Free PMC article.
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
Rescourio G, Gonzalez AZ, Jabri S, Belmontes B, Moody G, Whittington D, Huang X, Caenepeel S, Cardozo M, Cheng AC, Chow D, Dou H, Jones A, Kelly RC, Li Y, Lizarzaburu M, Lo MC, Mallari R, Meleza C, Rew Y, Simonovich S, Sun D, Turcotte S, Yan X, Wong SG, Yanez E, Zancanella M, Houze J, Medina JC, Hughes PE, Brown SP. Rescourio G, et al. Among authors: brown sp. J Med Chem. 2019 Nov 27;62(22):10258-10271. doi: 10.1021/acs.jmedchem.9b01310. Epub 2019 Nov 18. J Med Chem. 2019. PMID: 31736296
Optimization of GPR40 Agonists for Type 2 Diabetes.
Liu JJ, Wang Y, Ma Z, Schmitt M, Zhu L, Brown SP, Dransfield PJ, Sun Y, Sharma R, Guo Q, Zhuang R, Zhang J, Luo J, Tonn GR, Wong S, Swaminath G, Medina JC, Lin DC, Houze JB. Liu JJ, et al. Among authors: brown sp. ACS Med Chem Lett. 2014 Feb 6;5(5):517-21. doi: 10.1021/ml400501x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900872 Free PMC article.
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Brown SP, Dransfield PJ, Vimolratana M, Jiao X, Zhu L, Pattaropong V, Sun Y, Liu J, Luo J, Zhang J, Wong S, Zhuang R, Guo Q, Li F, Medina JC, Swaminath G, Lin DC, Houze JB. Brown SP, et al. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30. doi: 10.1021/ml300133f. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900539 Free PMC article.
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
Du X, Dransfield PJ, Lin DC, Wong S, Wang Y, Wang Z, Kohn T, Yu M, Brown SP, Vimolratana M, Zhu L, Li AR, Su Y, Jiao X, Liu JJ, Swaminath G, Tran T, Luo J, Zhuang R, Zhang J, Guo Q, Li F, Connors R, Medina JC, Houze JB. Du X, et al. Among authors: brown sp. ACS Med Chem Lett. 2014 Feb 3;5(4):384-9. doi: 10.1021/ml4005123. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900845 Free PMC article.
411 results