Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids  

作　　者：Hong Shan Liu Hu Ling Zheng Mei Ge Peng Xia Ying Chen 

机构地区：[1]Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China [2]Laiyi Biological Drug Research and Development Center Co., Ltd., Shanghai 201203, China

出　　处：《Chinese Chemical Letters》2011年第7期757-760,共4页中国化学快报（英文版）

基　　金：supported by grants from the National Natural Science Foundation of China awarded to P.Xia (No.20272010) and Y.Chen(No.30200348 and 30873164);the National Drug Innovative Program(No.2009ZX09301-011) for partial support

摘　　要：Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with ECs0 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with ECs0 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.

关 键 词：Pyrazo-annulated steroid 2-Methoxyestradiol （2-ME） VEGF inhibitory activity 

分 类 号：Q78[生物学—分子生物学] TQ457.29[化学工程—农药化工]