Discovery and optimization of 3-(2-(Pyrazolo [1, 5-a] pyrimidin-6-yl) ethynyl) benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1 …

…, J Luo, L Zhang, X Lu, Y Zhang, Z Zhang…

Index: Gao, Mingshan; Duan, Lei; Luo, Jinfeng; Zhang, Lianwen; Lu, Xiaoyun; Zhang, Yan; Zhang, Zhang; Tu, Zhengchao; Xu, Yong; Ren, Xiaomei; Ding, Ke Journal of Medicinal Chemistry, 2013 , vol. 56, # 8 p. 3281 - 3295

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Citation Number: 34

Abstract

Discoidin domain receptor 1 (DDR1) is an emerging potential molecular target for new anticancer drug discovery. We have discovered a series of 3-(2-(pyrazolo [1, 5-a] pyrimidin-6- yl) ethynyl) benzamides that are selective and orally bioavailable DDR1 inhibitors. The two most promising compounds (7rh and 7rj) inhibited the enzymatic activity of DDR1, with IC50 values of 6.8 and 7.0 nM, respectively, but were significantly less potent in suppressing ...