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

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. (C) 2020 Elsevier Masson SAS. All rights reserved.

Automated summary

A series of [1,3]thiazolo[4,5-e]isoindoles have been synthesized with high antiproliferative activity, with compound 11g showing the highest potency to induce cell cycle arrest and apoptosis. This compound could serve as a lead compound for new antimitotic drug discovery.