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33 results

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Page 1
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.
Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R. Boga SB, et al. Among authors: hruza a. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26. Bioorg Med Chem Lett. 2018. PMID: 29748051
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA. Boga SB, et al. Among authors: hruza aw. ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034615 Free PMC article.
Discovery of C-imidazole azaheptapyridine FPT inhibitors.
Zhu HY, Cooper AB, Desai J, Njoroge G, Kirschmeier P, Bishop WR, Strickland C, Hruza A, Doll RJ, Girijavallabhan VM. Zhu HY, et al. Among authors: hruza a. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1134-6. doi: 10.1016/j.bmcl.2009.12.013. Epub 2009 Dec 6. Bioorg Med Chem Lett. 2010. PMID: 20056542
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.
Deng Y, Shipps GW Jr, Zhao L, Siddiqui MA, Popovici-Muller J, Curran PJ, Duca JS, Hruza AW, Fischmann TO, Madison VS, Zhang R, McNemar CW, Mayhood TW, Syto R, Annis A, Kirschmeier P, Lees EM, Parry DA, Windsor WT. Deng Y, et al. Among authors: hruza aw. Bioorg Med Chem Lett. 2014 Jan 1;24(1):199-203. doi: 10.1016/j.bmcl.2013.11.041. Epub 2013 Nov 23. Bioorg Med Chem Lett. 2014. PMID: 24332088
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
Ho GD, Yang SW, Smotryski J, Bercovici A, Nechuta T, Smith EM, McElroy W, Tan Z, Tulshian D, McKittrick B, Greenlee WJ, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R. Ho GD, et al. Among authors: hruza a. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1019-22. doi: 10.1016/j.bmcl.2011.11.127. Epub 2011 Dec 9. Bioorg Med Chem Lett. 2012. PMID: 22222034
Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.
Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA. Morris EJ, et al. Among authors: hruza a. Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24. Cancer Discov. 2013. PMID: 23614898
Dissecting Therapeutic Resistance to ERK Inhibition.
Jha S, Morris EJ, Hruza A, Mansueto MS, Schroeder GK, Arbanas J, McMasters D, Restaino CR, Dayananth P, Black S, Elsen NL, Mannarino A, Cooper A, Fawell S, Zawel L, Jayaraman L, Samatar AA. Jha S, et al. Among authors: hruza a. Mol Cancer Ther. 2016 Apr;15(4):548-59. doi: 10.1158/1535-7163.MCT-15-0172. Epub 2016 Feb 1. Mol Cancer Ther. 2016. PMID: 26832798
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L. Yu T, et al. Among authors: hruza a. Bioorg Med Chem Lett. 2018 May 1;28(8):1397-1403. doi: 10.1016/j.bmcl.2018.02.037. Epub 2018 Feb 23. Bioorg Med Chem Lett. 2018. PMID: 29545102
33 results