丝裂霉素C和2-甲基氮丙啶的1a-甲酰基及1a-硫代甲酰基衍生物的合成与抗肿瘤活性

Synthesis and antineoplastic activity of 1a-formyl and 1a-thioformyl derivatives of mitomycin C and 2-methylaziridine.

作者信息

Fishbein P L, Kohn H

机构信息

Department of Chemistry, University of Houston, Texas 77004.

出版信息

J Med Chem. 1987 Oct;30(10):1767-73. doi: 10.1021/jm00393a015.

DOI:10.1021/jm00393a015

PMID:3116255

Abstract

A select number of 1-formyl- and 1-thioformyl-2-methylaziridine derivatives and the corresponding 1a-substituted mitomycin C analogues were synthesized and tested for antineoplastic activity by using an in vivo test with murine P388 leukemia. Select compounds were also tested in vivo with murine melanoma B16. Several of the mitomycin C derivatives displayed activity and some of the mitomycin C analogues were comparable in activity to the parent compound.

摘要

合成了一定数量的1-甲酰基-和1-硫代甲酰基-2-甲基氮丙啶衍生物以及相应的1a-取代丝裂霉素C类似物，并通过小鼠P388白血病体内试验测试其抗肿瘤活性。还对选定的化合物进行了小鼠黑色素瘤B16体内试验。几种丝裂霉素C衍生物表现出活性，一些丝裂霉素C类似物的活性与母体化合物相当。