吲哚衍生物作为 IsoCombretastatin A-4 类似物的抗癌特性。
Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues.
机构信息
Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France.
Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France.
出版信息
Eur J Med Chem. 2021 Nov 5;223:113656. doi: 10.1016/j.ejmech.2021.113656. Epub 2021 Jun 18.
In this study, a variety of original ligands related to Combretastatin A-4 and isoCombretastatin A-4, able to inhibit the tubulin polymerization into microtubules, was designed, synthesized, and evaluated. Our lead compound 15d having a quinazoline as A-ring and a 2-substituted indole as B-ring separated by a N-methyl linker displayed a remarkable sub-nanomolar level of cytotoxicity (IC < 1 nM) against 9 human cancer cell lines.
在这项研究中，设计、合成并评估了多种与 Combretastatin A-4 和 isoCombretastatin A-4 相关的原始配体，这些配体能抑制微管蛋白聚合为微管。我们的先导化合物 15d 具有一个作为 A 环的喹唑啉和一个作为 B 环的 2-取代吲哚，由一个 N-甲基连接子隔开，对 9 个人类癌细胞系显示出显著的亚纳摩尔水平的细胞毒性（IC < 1 nM）。
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