Identification of 4-(2-(4-amino-1, 2, 5-oxadiazol-3-yl)-1-ethyl-7-{[(3 S)-3-piperidinylmethyl] oxy}-1 H-imidazo [4, 5-c] pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a …

…, LV Lafrance, M Li, IG Safonov, DT Takata…

文献索引：Heerding, Dirk A.; Rhodes, Nelson; Leber, Jack D.; Clark, Tammy J.; Keenan, Richard M.; Lafrance, Louis V.; Li, Mei; Safonov, Igor G.; Takata, Dennis T.; Venslavsky, Joseph W.; Yamashita, Dennis S.; Choudhry, Anthony E.; Copeland, Robert A.; Lai, Zhihong; Schaber, Michael D.; Tummino, Peter J.; Strum, Susan L.; Wood, Edgar R.; Duckett, Derek R.; Eberwein, Derek; Knick, Victoria B.; Lansing, Timothy J.; McConnell, Randy T.; Zhang, ShuYun; Minthorn, Elisabeth A.; Concha, Nestor O.; Warren, Gregory L.; Kumar, Rakesh Journal of Medicinal Chemistry, 2008 , vol. 51, # 18 p. 5663 - 5679

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被引用次数: 88

摘要

Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of dominant negative AKT blocks the ability of a variety of growth factors to promote survival. Therefore, inhibitors of AKT kinase activity might be useful as monotherapy for the treatment of tumors with activated AKT. Herein, we describe our lead optimization studies culminating in the discovery of compound 3g (GSK690693). Compound 3g is a novel ATP competitive, ...