6533b860fe1ef96bd12c319e

RESEARCH PRODUCT

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

Ruoli BaiRoberta BortolozziVirginia SpanòAntonio Palumbo PiccionelloAlessandra MontalbanoErnest HamelPaola BarrajaMaria Valeria RaimondiRoberta RoccaStefano AlcaroGiampietro ViolaMarilia BarrecaAnna Carbone

subject

Models MolecularCell cycle checkpointIsoindoles1ApoptosisIsoindoles01 natural sciencesPolymerizationTubulin Polymerization InhibitorsCell cycle arrestHeLaStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundTubulinDrug DiscoveryHumansTubulin polymerization inhibitors030304 developmental biologyPharmacology0303 health sciencesDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistry3]thiazolo[4Organic ChemistryGeneral Medicinebiology.organism_classificationTubulin Modulators0104 chemical sciencesBiochemistrychemistryCell cultureApoptosis5-e]isoindoles13]thiazolo[45-e]isoindoles13]thiazolo[45-e]isoindoles; Apoptosis; Cell cycle arrest; Tubulin polymerization inhibitorsLead compoundDerivative (chemistry)HeLa Cells

description

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.

yearjournalcountryeditionlanguage
2021-01-01European Journal of Medicinal Chemistry
https://doi.org/10.1016/j.ejmech.2020.113122