哥纳香醇甲及其类似物的合成与抗肿瘤活性研究

哥纳香醇甲(1)是从番荔枝科哥纳香属植物海南哥纳香的根和茎皮中分离得到的有明显抗肿瘤活性的化合物,本文以α-D-葡庚糖酸内酯为原料,经9步反应对其进行了不对称合成研究,总收率为13.3%。根据药物设计原理,设计合成了26个类似物,并进行了抗肿瘤活性筛选,初步结果表明大部分化合物体外对多种瘤株有不同程度的抑制作用,其中部分化合物显示较强的活性。

STUDIES ON THE SYNTHESIS AND ANTITUMOR ACTIVITIES OF HOWIINOL A AND ITS ANALOGUES

Howiinol A(1), one of the active antitumor constituents from the root and stem bark of Goniothamus howii Meer. (Annonaceae) has been synthesized in nine steps from alpha-D-glucoheptonic gamma-lactone with an over all yield of 13.3%. It shows that all data of the synthetic product are identical to those of the natural howiinol A, thus the absolute configuration of natural howiinol A is further confirmed as 1. In the search for new antitumor compounds with high potency, 26 analogues have been synthesized. In pharmacological tests most of them showed antitumor activities in vitro, some of them are significant.