Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity
Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity
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发现具有有效抗肿瘤活性的吡唑啉酮螺环己二烯酮衍生物
DOI：
10.1016/j.bmcl.2019.126662
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发表时间：
2020
影响因子：
2.7
通讯作者：
Sheng Chunquan
中科院分区：
文献类型：
--
作者：
Wang Lei;Yang Zixuan;Ni Tianyu;Shi Wencai;Guo Yunbo;Li Keliang;Shi Anzhe;Wu Shanchao;Sheng Chunquan
以易得的吡唑四氢吡喃缩醛为原料，合成了一系列新的吡唑酮螺环己二酮衍生物，并测定了其抗肿瘤活性。化合物10s经鉴定具有良好的抗肿瘤活性。可浓度依赖性地诱导MDA-MB-231细胞凋亡，并使细胞周期主要停滞于G1期。
Starting from easy accessible pyrazoletetrahydropyran acetals, a series of new pyrazolone spirocyclohexadienone derivatives were synthesized and assayed for antitumor activity. Compound10swas identified to possess good antitumor activity. It could induce MDA-MB-231 cancer cell apoptosis in a concentration dependent manner and arrest the cell cycle progression mainly at the G1 phase.