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

Paola Barraja, Anna Carbone, Alessandra Montalbano, Maria Valeria Raimondi, Antonio Palumbo Piccionello, Marilia Barreca, Virginia Spano', Ernest Hamel, Roberta Bortolozzi, Roberta Rocca, Stefano Alcaro, Giampietro Viola, Ruoli Bai

Risultato della ricerca: Articlepeer review

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.
Lingua originaleEnglish
pagine (da-a)1-17
Numero di pagine17
RivistaEuropean Journal of Medicinal Chemistry
Volume212
Stato di pubblicazionePublished - 2021

All Science Journal Classification (ASJC) codes

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  • ???subjectarea.asjc.3000.3002???
  • ???subjectarea.asjc.1600.1605???

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