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. 2018 Feb 10;145:404-412.
doi: 10.1016/j.ejmech.2018.01.015. Epub 2018 Jan 6.

Synthesis and Biological Evaluation of 4-amino-5-cinnamoylthiazoles as Chalcone-Like Anticancer Agents

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Synthesis and Biological Evaluation of 4-amino-5-cinnamoylthiazoles as Chalcone-Like Anticancer Agents

Adileh Ayati et al. Eur J Med Chem. .

Abstract

A series of 4-amino-5-cinnamoylthiazoles 3a-p were designed and synthesized as chalcone-like anticancer agents. The synthesized derivatives 3a-p were evaluated for their in vitro antiproliferative activities against three different human cancer cell lines including MCF-7, HepG2 and SW480. Most of compounds could significantly prevent proliferation of tested cell lines. In particular, the pyrrolidine derivative 3e namely (E)-1-(4-amino-2-(pyrrolidin-1-yl)thiazol-5-yl)-3-(2,4-dichlorophenyl)prop-2-en-1-one showed promising activity, especially against HepG2 cells (IC50 = 10.6 μg/ml). Flow cytometric analyses revealed that the prototype compound 3e can prevent the proliferation of HepG2 cells by blockade of the cell cycle at the G2 phase and induction of apoptosis.

Keywords: Anticancer; Apoptosis; Chalcone; Cytotoxic activity; Thiazole.

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