论文部分内容阅读
目的设计并合成新型小分子Bcl-2蛋白抑制剂。方法基于已报道的活性小分子,运用Autodock4.2研究其与Bcl-2蛋白的作用模式,并以此设计、合成一系列新型小分子抑制剂,采用MTT法对人肝癌细胞Hep G-2进行体外抗肿瘤活性实验。结果设计合成了11个全新小分子化合物,其结构经~1HNMR和~(13)CNMR确定。结论化合物Ⅱ、Ⅴ、Ⅹ、Ⅺ有明显的体外抗肿瘤活性,化合物Ⅵ显示出比较好的体外抗肿瘤活性,高于阳性对照。
Objective To design and synthesize a novel small molecule Bcl-2 protein inhibitor. Methods Based on the reported small molecule activity, Autodock4.2 was used to study the mode of action of Bcl-2 protein. A series of novel small molecule inhibitors were designed and synthesized. Hep G-2 cells were treated with MTT In vitro anti-tumor activity experiment. Results Eleven new small molecule compounds were designed and synthesized. Their structures were confirmed by ~ 1HNMR and ~ (13) CNMR. Conclusion Compounds Ⅱ, Ⅴ, Ⅹ and Ⅺ have obvious antitumor activity in vitro. Compound Ⅵ shows better in vitro antitumor activity than the positive control.