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Synthesis and biological evaluation of 4-amino-5-cinnamoylthiazoles as chalcone-like anticancer agents

2018; Elsevier BV; Volume: 145; Linguagem: Inglês

10.1016/j.ejmech.2018.01.015

1768-3254

Adileh Ayati, Rezvan Esmaeili, Setareh Moghimi, Tayebeh Oghabi Bakhshaiesh, Zahra Eslami‐S, Keivan Majidzadeh‐A, Maliheh Safavi, Saeed Emami, Alireza Foroumadi,

Click Chemistry and Applications

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.