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.

Spano' V., Barreca M., Rocca R., Bortolozzi R., Bai R., Carbone A., et al. (2021). Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 212, 1-17 [10.1016/j.ejmech.2020.113122].

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

Spano' V.;Barreca M.;Carbone A.;Raimondi M. V.;Palumbo Piccionello A.;Montalbano A.
;
Barraja P.
2021-02-15

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.
https://www.sciencedirect.com/science/article/pii/S0223523420310941?via=ihub
Spano' V., Barreca M., Rocca R., Bortolozzi R., Bai R., Carbone A., et al. (2021). Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 212, 1-17 [10.1016/j.ejmech.2020.113122].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10447/460328
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