ZOU, XIAOQING,HYDER, SALMAN M.,LIANG, YAYUN,GRINTER, SAM Z,HUANG, SHENGYOU
申请号：
CA2822207
公开号：
CA2822207A1
申请日:
2011.12.22
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.
