Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters

被引：34

作者：

Koutsourea, Anna I. ^{[1
]}

Fousteris, Manolis A. ^{[1
]}

Arsenou, Evagelia S. ^{[1
]}

Papageorgiou, Athanasios ^{[2
]}

Pairas, George N. ^{[1
]}

Nikolaropoulos, Sotiris S. ^{[1
]}

机构：

[1] Univ Patras, Dept Pharm, Sch Hlth Sci, Med Chem Lab, Patras 26500, Greece

[2] Theagenion Anticanc Hosp, Lab Expt Chemotherapy, Thessaloniki, Greece

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 09期

关键词：

steroids; nitrogen mustards; antileukemic activity; SAR;

D O I：

10.1016/j.bmc.2008.03.015

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and the in vivo evaluation against leukemias P388 and L1210 of six new alkylating steroidal esters are described. The esteric derivatives incorporating the 17 beta-acetamido-B-lactamic steroidal skeleton exhibited increased antileukemic activity and lower toxicity, compared to the 17 beta-acetamido-7-keto analogs. Among the 17 beta-acetamido-B-lactamic steroidal esters, the most potent compound afforded four out of six cures in leukemia P388 and was measured to be almost non-toxic, producing significant low levels of toxicity. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5207 / 5215

页数：9

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