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.

设计并合成了一系列4-氨基-5-肉桂基噻唑3a-p，它们是类查尔酮样的抗癌药。评价了合成的衍生物3a-p对三种不同的人类癌细胞系包括MCF-7，HepG2和SW480的体外抗增殖活性。大多数化合物可以显着阻止受试细胞系的增殖。尤其是，吡咯烷衍生物3e，即（E）-1-（4-氨基-2-（吡咯烷-1-基）噻唑-5-基）-3-（2，4-二氯苯基）丙-2-烯- 1-one显示出有希望的活性，尤其是针对HepG2细胞（IC ₅₀  = 10.6μg/ ml）。流式细胞仪分析表明原型化合物3e 通过阻断G2期的细胞周期并诱导凋亡，可以阻止HepG2细胞的增殖。