Identification and Characterization of Novel Antimitotic Compounds for the Treatment of Breast Cancer
Abstract
Our goal is to find new antimitotic drugs for the treatment of breast cancer using a novel cell-based assay to screen natural product libraries and guide the purification of their active components. In year 1, we carried out a screen of over 30,000 extracts of terrestrial plants, algae and marine organisms, obtained 223 positive extracts, and isolated and identified active compounds from S of the positive extracts. In year 2, we isolated several new analogs of the microtubule-stabilizing compound eleutherobin and produced several more by synthetic transformation. We used the analogs to carry out an extended structure-activity relationship study of eleutherobin and identified unanticipated structural requirements that will be important for future pharmacophore models. We have also isolated sufficient amounts of eleutherobin and desmethyleleutherobin for in vivo testing. We isolated active compounds from 5 additional extracts, 3 of which have novel mechanisms of action that are currently under investigation.
Document Details
- Document Type
- Technical Report
- Publication Date
- Aug 01, 2001
- Accession Number
- ADA396413
Entities
People
- Michel Roberge
Organizations
- University of British Columbia