柔红霉素、5-亚氨基柔红霉素和阿霉素的N-烯胺衍生物的合成及其抗白血病活性

Synthesis and antileukemic activity of N-enamine derivatives of daunorubicin, 5-iminodaunorubicin, and doxorubicin.

作者信息

Stefańska B, Dzieduszycka M, Bontemps-Gracz M, Borowski E, Martelli S

机构信息

Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, Poland.

出版信息

J Antibiot (Tokyo). 1988 Feb;41(2):193-8. doi: 10.7164/antibiotics.41.193.

DOI:10.7164/antibiotics.41.193

PMID:3356607

Abstract

Eleven N-enamine derivatives of daunorubicin and of its 5-imino analogue as well as of doxorubicin have been synthesized and evaluated for antileukemic activity in vitro and in vivo. Comparison of biological activities of examined compounds with other enamine derivatives of daunorubicin, reported earlier by us, has indicated that the optimal activity is shown by N-(1-carboethoxypropen-1-yl-2)daunorubicin.

摘要

已合成了柔红霉素及其5-亚氨基类似物以及阿霉素的11种N-烯胺衍生物，并对其体外和体内抗白血病活性进行了评估。将所研究化合物的生物活性与我们之前报道的柔红霉素其他烯胺衍生物进行比较，结果表明N-(1-乙氧羰基丙烯-1-基-2)柔红霉素表现出最佳活性。