哥纳香醇甲类似物对KB瘤株的抑制作用的构效关系研究

Structure- activity rdatknship of Howiinol A in inhibition of KB cells

目的研究哥纳香醇甲的抗肿瘤活性构效关系。方法 经MTT法筛选了55个哥纳香醇甲类似物及中间体对KB瘤株的抑制作用。研究了以α-D-葡庚糖酸-δ-内酯为原料经9-10步合成的55个哥纳香醇甲类似物的抗KB瘤株活性与结构的关系。结果化合物9、11、21、25、34、38、44、49对KB瘤株的抑制作用强于哥纳香醇甲。结论哥纳香醇甲类似物8R构型、不饱和内酯及8位芳香酯为其活性的关键构型和基团。5,7-位的环状结构有利于增强活性。

Objective To study the structure-activity relationship of Howiinol A in inhibiting KB cell.Methods The antitumor activities of 55 derivatives of Howiinol A synthesized in nine (or ten) steps from α-D-glucoheptonic-δ-lactone were screened by MTT method.The structure - activity relationship of Howiinol A derivatives in inhibition of KB cells was reserched. Results The activities of compounds 9,21, 25,34,38,44 and 49 on KB cells were better than that of Howiinol A.Conclusions 8 R configuration of Howiinol A is active configuration. α,β-unsaturated-lactone is active group,and 5,7 - cyclic structure is conducive to enhancing their activities.