Isogoniotriol衍生物的合成及体外抑制肿瘤活性

Syntheses and antitumor activities of Isogoniotriol

目的 研究goniotriol抗肿瘤作用的构效关系。方法 以α D 葡庚糖酸 δ 内酯为原料经 9步反应 ,合成了 12个isogo niotriol衍生物 ,他们的结构经IR ,1H NMR ,MS和元素分析证实。经MTT法筛选了衍生物的抗肿瘤活性。结果 10个化合物(8b ,8c ,8d ,8e ,8f,9b ,9c ,9d ,9e ,9f)为新化合物 ,该类化合物 (8b ,8c,8f)体外对多种瘤株 (A2 780 ,HCT 8,Bel74 2 ,KB)抑制强度高于8(R) O 肉桂酰基 goniotriol,但化合物 (8d ,8e ,9b ,9c ,9d ,9e ,9f)抑制作用明显低于 8(R) O 肉桂酰基 goniotriol。结论 goniotriol衍生物的 8R构型为其活性的关键构型。

Aim To study the relationship of structure and its activities of goniotriol.Methods 12 derivatives of isogoniotriol have been synthesized in nine steps from α D glucoheptonic δ lactone.Their structures were confirmed by IR, 1H NMR,MS,element analyses.The antitumor activities of the compounds were screened by MTT methods.Results 10 derivatives of isogoniotriol(8b,8c,8d,8e,8f,9b,9c,9d,9e,9f) are new compounds.Pharmacological tests show that antitumor activities(A2780,HCT 8,Bel742,KB)of compounds (8b,8c,8f)were better but that of compounds(8d,8e,8f,9b,9c,9d,9e,9f)were lower than that of 8(R) O cinnamyl goniotriol in vitro.Conclusions 8R configuration of goniotriol was active configuration.