发明名称 |
Hydroxyphenstatin and the prodrugs thereof |
摘要 |
The benzophenone derivative of combretastatin A-1, designated "hydroxyphenstatin", was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted to a sodium phosphate prodrug by dibenzyl phosphite phosphorylation and subsequent benzyl cleavage: Hydroxyphenstatin and the prodrugs thereof were found to be a potent inhibitor of tubulin polymerization and to demonstrate surprisingly effective antineoplastic activity against a series of human cancer cells and murine P388 lymphocytic leukemia cells.
|
申请公布号 |
US6777578(B2) |
申请公布日期 |
2004.08.17 |
申请号 |
US20030258676 |
申请日期 |
2003.04.24 |
申请人 |
ARIZONA BOARD OF REGENTS |
发明人 |
PETTIT GEORGE R.;GREALISH MATTHEW P. |
分类号 |
A61K31/12;A61K31/38;A61K31/66;C07C45/29;C07C45/30;C07C45/45;C07C45/46;C07C45/67;C07C49/84;C07F9/12;(IPC1-7):C07C49/76;A01N35/00 |
主分类号 |
A61K31/12 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|