Discovery of new azaindole-based PI3K alpha inhibitors: Apoptotic and antiangiogenic effect on cancer cells

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Phosphatidylinositol-3-kinase alpha (PI3K alpha) 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 PI3K alpha 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 PI3K alpha inhibitors. Representative azaindole derivatives showed activity in a cellular proliferation and apoptosis assays. Moreover, B3 exhibited strong antiangiogenic effects on cancer cells. (C) 2010 Elsevier Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2010-12
Language
English
Article Type
Article
Keywords

PHOSPHOINOSITIDE 3-KINASE; POTENT; ANGIOGENESIS; KINASE; MUTATIONS; RAPAMYCIN; TARGET; PI3K; IDENTIFICATION; DERIVATIVES

Citation

BIOORGANIC MEDICINAL CHEMISTRY LETTERS, v.20, no.24, pp.7212 - 7215

ISSN
0960-894X
DOI
10.1016/j.bmcl.2010.10.108
URI
http://hdl.handle.net/10203/174455
Appears in Collection
CH-Journal Papers(저널논문)
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