发现具有强大抗肿瘤活性的新型双表水苏碱衍生物。
Discovery of novel bis-evodiamine derivatives with potent antitumor activity.
机构信息
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
出版信息
Bioorg Med Chem. 2022 Jul 1;65:116793. doi: 10.1016/j.bmc.2022.116793. Epub 2022 May 6.
Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.
受抗肿瘤天然产物吴茱萸碱的启发，设计并合成了一系列新型双吴茱萸碱衍生物，它们表现出很强的抗肿瘤活性。特别是化合物 13b 能有效抑制 HCT116 细胞的增殖和迁移。进一步的机制研究表明，化合物 13b 通过诱导 HCT116 细胞凋亡和将细胞周期阻滞在 G2/M 期来发挥作用。因此，化合物 13b 代表了一种有前途的新型抗肿瘤药物发现的先导化合物。
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