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

European journal of medicinal chemistry 2021 Feb 15

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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. Copyright © 2020 Elsevier Masson SAS. All rights reserved.

Citation

Virginia Spanò, Marilia Barreca, Roberta Rocca, Roberta Bortolozzi, Ruoli Bai, Anna Carbone, Maria Valeria Raimondi, Antonio Palumbo Piccionello, Alessandra Montalbano, Stefano Alcaro, Ernest Hamel, Giampietro Viola, Paola Barraja. Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors. European journal of medicinal chemistry. 2021 Feb 15;212:113122