De A U, Saha B P
J Pharm Sci. 1975 Feb;64(2):49-5.
A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provided by some hypoglycemic Vinca alkaloids, such as vincamine, vindoline, and vindolinine, having the indolizine ring as one structural component. But an extension of the rationale that indolizines are also the structural components of some carcinolytic Vinca alkaloids, such as vincristine and vinblastine, used in cancer chemotherapy provided encouraging results. One indolizine derivative showed significant antineoplastic activity in Ehrlich ascites carcinoma.
合成了几种1,2-双（N-烷基氨甲基）中氮茚、简单的中氮茚羧酸以及几种6-烷氧基中氮茚-2-羧酸，并将其作为可能的口服降糖药进行筛选。由于缺乏任何显著的降糖活性，这些化合物被排除在某些降糖长春花生物碱（如长春胺、长春多灵和长春多宁）所提供的预测结构先导之外，这些生物碱以中氮茚环作为一个结构成分。但是，基于中氮茚也是一些用于癌症化疗的溶癌长春花生物碱（如长春新碱和长春碱）的结构成分这一理论进行拓展，得到了令人鼓舞的结果。一种中氮茚衍生物在艾氏腹水癌中显示出显著的抗肿瘤活性。
