Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using "click" chemistry.
Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using "click" chemistry.
复制标题
DOI：
10.1039/c2ob25902h
复制
发表时间：
2012-11-14
影响因子：
3.2
通讯作者：
Croy RG
中科院分区：
文献类型：
--
作者：
Hanson RN;Hua E;Labaree D;Hochberg RB;Proffitt K;Essigmann JM;Croy RG
A convergent synthesis of a novel estrogen receptor-targeted drug hybrid was developed based on structures of the potent anti-proliferative mitomycin C and the steroidal anti-estrogen RU 39411. The steroidal antiestrogen was prepared with an azido-triethylene glycoloxy linker while the mitomycin C derivative (porfirimycin) incorporated a complementary 7-N-terminal alkyne. The two components were ligated using the Huisgen [3 + 2] cycloaddition (“click”) reaction. Preliminary biological assays demonstrated that the final hybrid compound retained both potent anti-estrogenic and anti-proliferative activities.
登录
查看更多内容
影响因子：
3.6
作者：
Agouridas, V;Blazejewski, JC;Popkin, ME
通讯作者：
Popkin, ME
影响因子：
5.5
作者：
Fernandez-Megia, E;Correa, J;Riguera, R
通讯作者：
Riguera, R
影响因子：
64.8
作者：
GREEN, S;WALTER, P;CHAMBON, P
通讯作者：
CHAMBON, P
DOI：
10.1016/0960-0760(92)90392-v
发表时间：
1992-03-01
影响因子：
4.1
作者：
CLAUSSNER, A;NEDELEC, L;VANDEVELDE, P
通讯作者：
VANDEVELDE, P
影响因子：
5.1
作者：
EISENBRAND, G;FISCHER, J;ZELEZNY, O
通讯作者：
ZELEZNY, O