Synthesis and biological evaluation of novel steroid-linked nitrogen mustards  

作　　者：Hua Bing Zhang Ji Jun Xue Xiao Long Zhao De Gang Liu Ying Li 

机构地区：[1]State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China

出　　处：《Chinese Chemical Letters》2009年第6期680-683,共4页中国化学快报（英文版）

基　　金：support of the National Natural Science Foundation of China(No.20672050)

摘　　要：Two novel steroid-linked nitrogen mustard conjugates la and lb were synthesized by using estrogenic acid 4 coupled with aniline mustard 8 and phenol mustard 13 in an esterification or amidation procedure. Preliminary cytotoxic screening on cancer cell lines in vitro showed that, the steroid-ester linked nitrogen mustard conjugate la exhibited obvious increasing of activities.Two novel steroid-linked nitrogen mustard conjugates la and lb were synthesized by using estrogenic acid 4 coupled with aniline mustard 8 and phenol mustard 13 in an esterification or amidation procedure. Preliminary cytotoxic screening on cancer cell lines in vitro showed that, the steroid-ester linked nitrogen mustard conjugate la exhibited obvious increasing of activities.

关 键 词：STEROID Nitrogen mustards SYNTHESIS Biological activity 

分 类 号：Q959.482[生物学—动物学] X826[环境科学与工程—环境工程]