Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799

…, T Miyazaki, K Morikami, K Yoshinari, M Yoshida…

Index: Ohwada, Jun; Ebiike, Hirosato; Kawada, Hatsuo; Tsukazaki, Masao; Nakamura, Mitsuaki; Miyazaki, Takuya; Morikami, Kenji; Yoshinari, Kiyoshi; Yoshida, Miyuki; Kondoh, Osamu; Kuramoto, Shino; Ogawa, Kotaro; Aoki, Yuko; Shimma, Nobuo Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1767 - 1772

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Citation Number: 36

Abstract

Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was ...