丝裂霉素的6-取代丝裂烯类似物的合成及生物活性

Synthesis and biological activity of 6-substituted mitosene analogues of the mitomycins.

作者信息

Casner M L, Remers W A, Bradner W T

出版信息

J Med Chem. 1985 Jul;28(7):921-6. doi: 10.1021/jm00145a013.

Abstract

A series of 1-acetoxymitosene analogues, in which the substituent at C-6 was varied, was prepared by total synthesis and screened for activity against P388 leukemia in mice and induction of lambda phage in Escherichia coli. Among the 6-substituents prepared, none was as effective as the methyl group in conferring biological activity. However, certain N-methylcarbamates were more active than the unsubstituted carbamates.

摘要

通过全合成制备了一系列C-6位取代基不同的1-乙酰氧基米托蒽醌类似物，并对其针对小鼠P388白血病的活性以及在大肠杆菌中诱导λ噬菌体的能力进行了筛选。在所制备的6-取代基中，没有一个在赋予生物活性方面像甲基那样有效。然而，某些N-甲基氨基甲酸酯比未取代的氨基甲酸酯更具活性。