抗癌及癌化学预防药物的研究:3-α-酮醛香豆素衍生物的合成及其抗致突活性与结构间的关系

α-酮醛及其衍生物在抗病毒、抗肿瘤方面有一定活性。我们合成了18个新的3-α-酮醛香豆素衍生物,研究该类化合物的质谱裂解方式与氢核磁共振谱的特征峰。体外药理筛选发现其中部分化合物有不同程度的抗致突活性,对其构效关系进行了分析,并提出了这类化合物产生抗致突活性的可能亚结构。

STUDIES OF ANTITUMOR AND CHEMOPREVENTIVE AGENTS AGAINST NEOPLASM: SYNTHESIS OF COUMARIN 3-GLYOXAL DERIVATIVES AND RELATIONSHIP BETWEEN STRUCTURE AND ANTIMUTAGENIC ACTIVITY

It has been shown that α-glyoxal and its derivatives possess antivirus and antitumor activities. Eighteen new coumarin 3-glyoxal derivatives were synthesized in our laboratory. The fragmentation pattern of MS and the characteristic signals of ¹HNMR of these compounds have also been studied. In pharmacological test in vitro most of these analogues showed antimutagenic activities, among them, compound 9 exhibited very strong antimutagenic activity and eight compounds showed strong effects. The struture activity relationship and the possible active substructure responsible for the activity of these compounds were discussed. As expected, coumarin 3-glyoxals showed higher antimutagenic activities than their 3-acetyl coumarin counterparts . We also found that alkylation or esterification of 7-hydroxy were favorable to their activities .