EC144 is a potent inhibitor of the heat shock protein 90

J Shi, R Van de Water, K Hong, RB Lamer…

文献索引：Shi, Jiandong; Van De Water, Ryan; Hong, Kevin; Lamer, Ryan B.; Weichert, Kenneth W.; Sandoval, Cristina M.; Kasibhatla, Srinivas R.; Boehm, Marcus F.; Chao, Jianhua; Lundgren, Karen; Timple, Noelito; Lough, Rachel; Ibanez, Gerardo; Boykin, Christina; Burrows, Francis J.; Kehry, Marilyn R.; Yun, Theodore J.; Harning, Erin K.; Ambrose, Christine; Thompson, Jeffrey; Bixler, Sarah A.; Dunah, Anthone; Snodgrass-Belt, Pamela; Arndt, Joseph; Enyedy, Istvan J.; Li, Ping; Hong, Victor S.; McKenzie, Andres; Biamonte, Marco A. Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7786 - 7795

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被引用次数: 18

摘要

Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3, 5-dimethylpyridin-2-yl) methyl)-7 H-pyrrolo [2, 3-d] pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro and in vivo than the first generation inhibitor 14 (BIIB021) that completed phase II clinical trials. Alkyne 40 is more potent than 14 in an Hsp90α binding assay (IC50= 1.1 vs 5.1 nM) as well as in its ...