A set of 20 2-cyanoaziridine-1-carboxamides was synthesized from 2-cyanoaziridine and appropriate isocyanates. These compounds were active against a variety of solid and hematological tumor cells in culture, including strains resistant to doxorubicin and mitoxantrone. Their potencies in these assays correlated with the lipophilicity of substituents. The N-phenyl derivative was more potent and equally effective to imexon, a cyclized 2-cyanoaziridine-1-carboxamide of clinical interest, against cloned fresh human tumors.
Disclosed are novel compositions comprising a lipid and imexon or a derivative thereof. Also disclosed are liposomal compositions comprising imexon or a derivative thereof. Methods for administrating pharmaceutically acceptable compositions comprising a lipid and imexon or a derivative thereof for the treatment of diseases, such as cancer, are also disclosed herein.
申请人:THE ARIZONA BOARD OF REGENTS, ON BEHALF OF THE UNIVERSITY OF ARIZONA
公开号:EP1027041A1
公开(公告)日:2000-08-16
EP1027041A4
申请人:——
公开号:EP1027041A4
公开(公告)日:2001-06-13
US6297230B1
申请人:——
公开号:US6297230B1
公开(公告)日:2001-10-02
[EN] NOVEL CYANOAZIRIDINES FOR TREATING CANCER<br/>[FR] NOUVELLES CYANOAZIRIDINES POUR TRAITER LE CANCER
申请人:ARIZONA BOARD OF REGENTS, UNIVERSITY OF ARIZONA
公开号:WO1999000120A1
公开(公告)日:1999-01-07
(EN) This invention relates to novel cyanoaziridines for treatment of cancer.(FR) La présente invention concerne de nouvelles cyanoaziridines destinées au traitement du cancer.