Discovery of new azaindole-based PI3Kα inhibitors: Apoptotic and antiangiogenic effect on cancer cells

S Hong, S Lee, B Kim, H Lee, SS Hong…

Index: Hong, Seunghee; Lee, Soyoung; Kim, Bomi; Lee, Hyunseung; Hong, Soon-Sun; Hong, Sungwoo Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7212 - 7215

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Citation Number: 30

Abstract

Phosphatidylinositol-3-kinase alpha (PI3Kα) is an important target in cancer due to the deregulation of the PI3K/AKT signaling pathway in many tumors. In this study, we designed [3, 5-d]-7-azaindole analogs as PI3Kα inhibitors through the fragment-growing strategy. By varying groups at the 3, 5-positions of azaindole, we developed the SAR (Structure–activity relationship) and identified a series of potent PI3Kα inhibitors. Representative azaindole ...