NDLI: Diversity through semisynthesis: the chemistry and biological activity of semisynthetic epothilone derivatives

Content Provider	Springer Nature Link
Author	Altmann, Karl Heinz Gaugaz, Fabienne Z. Schiess, Raphael
Copyright Year	2010
Abstract	Epothilones are myxobacterial natural products that inhibit human cancer cell growth through the stabilization of cellular microtubules (i.e., a “taxol-like” mechanism of action). They have proven to be highly productive lead structures for anticancer drug discovery, with at least seven epothilone-type agents having entered clinical trials in humans over the last several years. SAR studies on epothilones have included a large number of fully synthetic analogs and semisynthetic derivatives. Previous reviews on the chemistry and biology of epothilones have mostly focused on analogs that were obtained by de novo chemical synthesis. In contrast, the current review provides a comprehensive overview on the chemical transformations that have been investigated for the major epothilones A and B as starting materials, and it discusses the biological activity of the resulting products. Many semisynthetic epothilone derivatives have been found to exhibit potent effects on human cancer cell growth and several of these have been advanced to the stage of clinical development. This includes the epothilone B lactam ixabepilone (Ixempra$^{®}$, which has been approved by the FDA for the treatment of advanced and metastatic breast cancer.
Starting Page	383
Ending Page	399
Page Count	17
File Format	PDF
ISSN	13811991
Journal	Molecular Diversity
Volume Number	15
Issue Number	2
e-ISSN	1573501X
Language	English
Publisher	Springer Netherlands
Publisher Date	2011-01-01
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Cancer Drug discovery Epothilones Microtubules Natural products SAR Semisynthesis Review Pharmacy Polymer Sciences Biochemistry Organic Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Medicine Drug Discovery Molecular Biology Physical and Theoretical Chemistry Information Systems Catalysis Inorganic Chemistry

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