专利检索 ap:("ARIZONA BOARD OF REGENTS, A BODY CORPORATE OF THE STATE OF ARIZONA acting for AND on behalf of ARIZONA STATE UNIVERSITY") AND inv:"TOKI, Brian" 第 1 页

1.

发明公开
SYNTHESIS OF PHENSTATIN AND PRODRUGS THEREOF 审中-公开
标题翻译：合成PHENSTATIN及其前体药物

公开(公告)号：EP1045689A1

公开(公告)日：2000-10-25

申请号：EP99902133.0

申请日：1999-01-09

申请人： ARIZONA BOARD OF REGENTS, A BODY CORPORATE OF THE STATE OF ARIZONA acting for and on behalf of ARIZONA STATE UNIVERSITY

发明人： PETTIT, George, R. , TOKI, Brian

IPC分类号： A61K31/09 , A61K31/075 , A61K31/66 , C07C43/215 , C07C217/80

CPC分类号： A61K31/661 , A61K31/122 , C07C49/84 , C07C69/017 , C07F9/12

摘要： A newly discovered antineoplastic compound denominated 'phenstatin' is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).