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Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).
Come JH, Collier PN, Henderson JA, Pierce AC, Davies RJ, Le Tiran A, O'Dowd H, Bandarage UK, Cao J, Deininger D, Grey R, Krueger EB, Lowe DB, Liang J, Liao Y, Messersmith D, Nanthakumar S, Sizensky E, Wang J, Xu J, Chin EY, Damagnez V, Doran JD, Dworakowski W, Griffith JP, Jacobs MD, Khare-Pandit S, Mahajan S, Moody CS, Aronov AM. Come JH, et al. Among authors: jacobs md. J Med Chem. 2018 Jun 28;61(12):5245-5256. doi: 10.1021/acs.jmedchem.8b00085. Epub 2018 Jun 14. J Med Chem. 2018. PMID: 29847724
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X. Aronov AM, et al. Among authors: jacobs m. J Med Chem. 2007 Mar 22;50(6):1280-7. doi: 10.1021/jm061381f. Epub 2007 Feb 15. J Med Chem. 2007. PMID: 17300186
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Markland W, Namchuk MN, Nanthakumar S, Poondru S, Straub J, ter Haar E, Xie X. Aronov AM, et al. Among authors: jacobs m. J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q. J Med Chem. 2009. PMID: 19827834
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: jacobs m, jacobs dh. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Boyd MJ, Bandarage UK, Bennett H, Byrn RR, Davies I, Gu W, Jacobs M, Ledeboer MW, Ledford B, Leeman JR, Perola E, Wang T, Bennani Y, Clark MP, Charifson PS. Boyd MJ, et al. Among authors: jacobs m. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. doi: 10.1016/j.bmcl.2015.03.013. Epub 2015 Mar 14. Bioorg Med Chem Lett. 2015. PMID: 25827523
3,784 results