Molecules, Vol. 22, Pages 2005: New Tripentone Analogs with Antiproliferative Activity
Molecules, Vol. 22, Pages 2005: New Tripentone Analogs with Antiproliferative Activity
Molecules doi: 10.3390/molecules22112005
Authors:
Barbara Parrino
Salviana Ullo
Alessandro Attanzio
Virginia Spanò
Stella Cascioferro
Alessandra Montalbano
Paola Barraja
Luisa Tesoriere
Girolamo Cirrincione
Patrizia Diana
Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 and MCF-7 cells, respectively, did not affect the viability of Caco-2 differentiated in normal intestinal-like cells, suggesting tumor cells as the main target of its cytotoxic action. The same compound was further investigated in order to study its mode of action. Results showed that it did not exert necrotic effects, while induced a clear shift of viable cells towards early apoptosis. Flow cytometric analysis demonstrated that this compound caused cell ...
Source: Molecules - Category: Chemistry Authors: Barbara Parrino Salviana Ullo Alessandro Attanzio Virginia Span ò Stella Cascioferro Alessandra Montalbano Paola Barraja Luisa Tesoriere Girolamo Cirrincione Patrizia Diana Tags: Article Source Type: research
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