2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate:: A potent antitumor agent

被引：7

作者：

Huang, ZH

Yang, GJ

Lin, ZL

Huang, JL ^{[1
]}

机构：

[1] Fudan Univ, Dept Macromol Sci, Educ Minist China, Key Lab Mol Engn Polymers, Shanghai 200433, Peoples R China

[2] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(01)00157-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-[N-1-2-Pyrimidyl-aminobenzensulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate has been prepared by reaction of chlorambucil with sulfadiazine derivative. Schiff's base has been used as the protective group of the;aromatic amine in the synthesis. It can be completely removed by the irradiation of 365 nm UV light at room temperature. The title compound exhibits a high antitumor activity with a therapeutic index (TI) of 47.55 which is twice that of chlorambucil's (TI: 22.84). (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1099 / 1103

页数：5

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