Chengze Tian, Chen-Yui Yang, Tianze Wu
Jul 17, 2021
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Influential Citations
8
Citations
Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymatic and cellular activities. Most compounds displayed nanomolar inhibitory activities against PI3Ks, among which 25 displayed high LLE and micromolar inhibitory potency against three human tumor cell lines (IC50 = 0.264 μM, 2.04 μM, 1.14 μM).