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Page 1
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
Lin H, Yamashita DS, Zeng J, Xie R, Wang W, Nidarmarthy S, Luengo JI, Rhodes N, Knick VB, Choudhry AE, Lai Z, Minthorn EA, Strum SL, Wood ER, Elkins PA, Concha NO, Heerding DA. Lin H, et al. Among authors: yamashita ds. Bioorg Med Chem Lett. 2010 Jan 15;20(2):673-8. doi: 10.1016/j.bmcl.2009.11.064. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20006497
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: yamashita ds. J Med Chem. 2008 Sep 25;51(18):5663-79. doi: 10.1021/jm8004527. J Med Chem. 2008. PMID: 18800763
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Lin H, Yamashita DS, Zeng J, Xie R, Verma S, Luengo JI, Rhodes N, Zhang S, Robell KA, Choudhry AE, Lai Z, Kumar R, Minthorn EA, Brown KK, Heerding DA. Lin H, et al. Among authors: yamashita ds. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. doi: 10.1016/j.bmcl.2009.11.060. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20005102
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. Among authors: yamashita ds. 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
Azepanone-based inhibitors of human cathepsin L.
Marquis RW, James I, Zeng J, Trout RE, Thompson S, Rahman A, Yamashita DS, Xie R, Ru Y, Gress CJ, Blake S, Lark MA, Hwang SM, Tomaszek T, Offen P, Head MS, Cummings MD, Veber DF. Marquis RW, et al. Among authors: yamashita ds. J Med Chem. 2005 Nov 3;48(22):6870-8. doi: 10.1021/jm0502079. J Med Chem. 2005. PMID: 16250645
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF. Yamashita DS, et al. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577
28 results