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Page 1
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Yang H, Medeiros PF, Raha K, Elkins P, Lind KE, Lehr R, Adams ND, Burgess JL, Schmidt SJ, Knight SD, Auger KR, Schaber MD, Franklin GJ, Ding Y, DeLorey JL, Centrella PA, Mataruse S, Skinner SR, Clark MA, Cuozzo JW, Evindar G. Yang H, et al. Among authors: schaber md. ACS Med Chem Lett. 2015 Mar 20;6(5):531-6. doi: 10.1021/acsmedchemlett.5b00025. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005528 Free PMC article.
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
Lin H, Schulz MJ, Xie R, Zeng J, Luengo JI, Squire MD, Tedesco R, Qu J, Erhard K, Mack JF, Raha K, Plant R, Rominger CM, Ariazi JL, Sherk CS, Schaber MD, McSurdy-Freed J, Spengler MD, Davis CB, Hardwicke MA, Rivero RA. Lin H, et al. Among authors: schaber md. ACS Med Chem Lett. 2012 May 29;3(7):524-9. doi: 10.1021/ml300045b. eCollection 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 24900504 Free PMC article.
Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.
Lin H, Erhard K, Hardwicke MA, Luengo JI, Mack JF, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Sanchez RM, Schaber MD, Schulz MJ, Spengler MD, Tedesco R, Xie R, Zeng JJ, Rivero RA. Lin H, et al. Among authors: schaber md. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2230-4. doi: 10.1016/j.bmcl.2012.01.092. Epub 2012 Feb 4. Bioorg Med Chem Lett. 2012. PMID: 22361133
Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.
Sanchez RM, Erhard K, Hardwicke MA, Lin H, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Schaber MD, Spengler MD, Moore ML, Yu H, Luengo JI, Tedesco R, Rivero RA. Sanchez RM, et al. Among authors: schaber md. Bioorg Med Chem Lett. 2012 May 1;22(9):3198-202. doi: 10.1016/j.bmcl.2012.03.039. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22475557
Aminofurazans as potent inhibitors of AKT kinase.
Rouse MB, Seefeld MA, Leber JD, McNulty KC, Sun L, Miller WH, Zhang S, Minthorn EA, Concha NO, Choudhry AE, Schaber MD, Heerding DA. Rouse MB, et al. Among authors: schaber md. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. doi: 10.1016/j.bmcl.2009.01.002. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19179070
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R. Heerding DA, et al. Among authors: schaber md. J Med Chem. 2008 Sep 25;51(18):5663-79. doi: 10.1021/jm8004527. J Med Chem. 2008. PMID: 18800763
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.
Lin H, Yamashita DS, Xie R, Zeng J, Wang W, Leber J, Safonov IG, Verma S, Li M, Lafrance L, Venslavsky J, Takata D, Luengo JI, Kahana JA, Zhang S, Robell KA, Levy D, Kumar R, Choudhry AE, Schaber M, Lai Z, Brown BS, Donovan BT, Minthorn EA, Brown KK, Heerding DA. Lin H, et al. Bioorg Med Chem Lett. 2010 Jan 15;20(2):684-8. doi: 10.1016/j.bmcl.2009.11.061. Epub 2009 Dec 16. Bioorg Med Chem Lett. 2010. PMID: 20006500
N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.
Williams TM, Bergman JM, Brashear K, Breslin MJ, Dinsmore CJ, Hutchinson JH, MacTough SC, Stump CA, Wei DD, Zartman CB, Bogusky MJ, Culberson JC, Buser-Doepner C, Davide J, Greenberg IB, Hamilton KA, Koblan KS, Kohl NE, Liu D, Lobell RB, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Huff JR, et al. Williams TM, et al. Among authors: schaber md. J Med Chem. 1999 Sep 23;42(19):3779-84. doi: 10.1021/jm990254z. J Med Chem. 1999. PMID: 10508426 No abstract available.
52 results