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[1,3]噻唑并[4,5-e]异吲哚啉作为微管蛋白聚合抑制剂的研究进展。

Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors.

机构信息

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.

Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia di Catanzaro, Viale Europa, 88100, Catanzaro, Italy; Net4Science srl, Academic Spinoff, Università Magna Græcia di Catanzaro, Viale Europa, 88100, Catanzaro, Italy.

出版信息

Eur J Med Chem. 2021 Feb 15;212:113122. doi: 10.1016/j.ejmech.2020.113122. Epub 2020 Dec 24.

DOI:10.1016/j.ejmech.2020.113122
PMID:33401199
Abstract

A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs.

摘要

通过一种通用且高产的多步序列，合成了一系列[1,3]噻唑并[4,5-e]异吲哚。对新化合物在全 NCI 人类肿瘤细胞系面板上的抗增殖活性进行评估，突出了几种能够以微摩尔亚微摩尔浓度抑制肿瘤细胞增殖的化合物。最活跃的衍生物 11g 被发现能够使 HeLa 细胞中的细胞周期停滞在 G2/M 期，并通过线粒体途径诱导细胞凋亡，使其成为发现新的抗有丝分裂药物的先导化合物。

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