abstract |
The present invention identifies a cholesterol biosynthetic pathway involving the enzyme oxidosqualene cyclase as a novel protein target for anti-tumor therapy. Furthermore, the present invention provides a group of oxidosqualene cyclase inhibitors containing a tertiary amine linked to an aromatic ring structure as a novel anticancer agent. The compounds described herein include breast cancer cells, prostate cancer cells, lung cancer cells (including drug resistant lung cancer H69AR), colon cancer cells, ovarian cancer cells (including drug resistant OVCAR-3), and pancreatic cancer cells. Nineteen cell lines and human breast and prostate xenograft tumor growth were tested and shown to have activity. |