School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China.
Central Laboratory, The NO.1 Affiliated Hospital of Yunnan University of Chinese Medicine, Kunming 650021, PR China.
Bioorg Med Chem Lett. 2023 Jul 15;91:129378. doi: 10.1016/j.bmcl.2023.129378. Epub 2023 Jun 16.
In this work, a series of novel benzofuran derivatives linked to dipiperazine moiety have been prepared, and in vitro anticancer activity against Hela and A549 was investigated. The results demonstrated that benzofuran derivatives exerted potent antitumor effect. Especially, compounds 8c and 8d showed better antitumor activity against A549 (IC = 0.12 μM and 0.43 μM). Further mechanism study indicated that compound 8d could significantly induce cell apoptosis in A549 by FACs analysis.
在这项工作中，合成了一系列连接哌嗪部分的新型苯并呋喃衍生物，并对其在体外对 Hela 和 A549 的抗癌活性进行了研究。结果表明，苯并呋喃衍生物具有很强的抗肿瘤作用。特别是化合物 8c 和 8d 对 A549 的抗肿瘤活性更好（IC = 0.12 μM 和 0.43 μM）。进一步的机制研究表明，化合物 8d 通过 FACs 分析可以显著诱导 A549 细胞凋亡。
