Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373362 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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 derivatives showed activity in a cellular proliferation and apoptosis assays. Moreover, B3 exhibited strong antiangiogenic effects on cancer cells.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Seunghee Hong, Soyoung Lee, Bomi Kim, Hyunseung Lee, Soon-Sun Hong, Sungwoo Hong,