Discovery and optimization of 2-(4-substituted-pyrrolo [2, 3-b] pyridin-3-yl) methylene-4-hydroxybenzofuran-3 (2H)-ones as potent and selective ATP-competitive …

…, I Hollander, TS Mansour, S Ayral-Kaloustian…

文献索引：Tsou, Hwei-Ru; MacEwan, Gloria; Birnberg, Gary; Grosu, George; Bursavich, Matthew G.; Bard, Joel; Brooijmans, Natasja; Toral-Barza, Lourdes; Hollander, Irwin; Mansour, Tarek S.; Ayral-Kaloustian, Semiramis; Yu, Ker Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 7 p. 2321 - 2325

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被引用次数: 22

摘要

We discovered 2-(4-substituted-pyrrolo [2, 3-b] pyridin-3-yl) methylene-4-hydroxybenzofuran- 3 (2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Since phenolic OH groups pose metabolic liability, one of the two hydroxyl groups was selectively removed. The SAR data showed the structural features necessary for subnanomolar inhibitory activity against mTOR kinase as well as selectivity ...