【摘 要】
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A series of novel chromeno[4,3-c]pyrazol-4(2H)-one containing carbonyl or oxime derivatives(4a-4n,5a-5n)have been synthesized and evaluated their biological activities as PI3K inhibitors.Out of them,c
【机 构】
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State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,People's Rep
【出 处】
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第八届国际分子模拟与信息技术应用学术会议
论文部分内容阅读
A series of novel chromeno[4,3-c]pyrazol-4(2H)-one containing carbonyl or oxime derivatives(4a-4n,5a-5n)have been synthesized and evaluated their biological activities as PI3K inhibitors.Out of them,compound 5l showed the most potent antiproliferative activities against HCT-116 with IC50 of 0.10 μM in vitro,and exhibited the most potent activity for PI3Kα with the value of 0.012 μM.Docking simulation of 51 into PI3Kα active site were performed to determine the probable binding model,and it indicated that compound 5l could be optimized as a potential inhibitor of PI3Kα in the further study.
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