Second-generation epothilones: Discovery of fludelone and its extraordinary antitumor properties Journal Article
| Authors: | Cho, Y. S.; Wu, K. D.; Moore, M. A. S.; Chou, T. C.; Danishefsky, S. J. |
| Article Title: | Second-generation epothilones: Discovery of fludelone and its extraordinary antitumor properties |
| Abstract: | Herein, we describe the development of the second generation of epothilone derivatives, which possess impressive preclinical antitumor properties. In particular, we focus on the discovery and biological evaluation of a trifluoromethyl-9,10-dehydroepothilone derivative, termed fludelone, to which we gained access through diverted total synthesis. This review serves to highlight the role of natural product-based research combined with the power of chemical synthesis in the discovery and development of valuable drug candidates. Copyright © 2005 Prous Science. |
| Keywords: | unclassified drug; review; nonhuman; paclitaxel; binding affinity; cell cycle; cell growth; weight reduction; in vivo study; antineoplastic activity; cancer cell culture; cytotoxicity; drug structure; in vitro study; drug synthesis; structure activity relation; cancer inhibition; toxicity testing; lymphatic leukemia; colon carcinoma; ic 50; drug binding; drug stability; epothilone a; epothilone b; epothilone derivative; growth inhibition; fludelone; 12,13 desoxy epothilone b; 9,10 dehydro epothilone b |
| Journal Title: | Drugs of the Future |
| Volume: | 30 |
| Issue: | 7 |
| ISSN: | 0377-8282 |
| Publisher: | Prous Science |
| Date Published: | 2005-01-01 |
| Start Page: | 737 |
| End Page: | 745 |
| Language: | English |
| DOI: | 10.1358/dof.2005.030.07.895806 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 16" - "Export Date: 24 October 2012" - "CODEN: DRFUD" - "Source: Scopus" |
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29Wu -
12
Cho -
539Danishefsky -
318Chou -
549Moore
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