| Literature DB >> 28688277 |
Barbara Parrino1, Alessandro Attanzio1, Virginia Spanò1, Stella Cascioferro1, Alessandra Montalbano1, Paola Barraja1, Luisa Tesoriere1, Patrizia Diana1, Girolamo Cirrincione1, Anna Carbone2.
Abstract
A new series of thiazole nortopsentin analogues was conveniently synthesized with fair overall yields. The antiproliferative activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. Four of them showed good antitumor activity with GI50 values from micro to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and DNA fragmentation. The most active and selective of the new thiazoles confined viable cells in G2/M phase and markedly inhibited in vitro CDK1 activity.Entities:
Keywords: Antiproliferative activity; Apoptosis; CDK1 inhibitors; Marine alkaloids; Nortopsentin analogues; Thiazolyl-1H-pyrrolo[2,3-b]pyridines
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Year: 2017 PMID： 28688277 DOI： 10.1016/j.ejmech.2017.06.052
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514