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Scientists at The Scripps Research Institute Synthesize Potential New Anti-Cancer Compounds

May 15, 1997- La Jolla, CA. - Scientists at The Scripps Research Institute (TSRI) who were the first to publish a total chemical synthesis of the anti-cancer agent, Taxol , have synthesized another naturally occurring compound that may have some advantages over that chemotherapeutic agent for ovarian cancer.

In a paper published today in Nature, a group led by K.C. Nicolaou, Ph.D., Darlene Shiley Chair, Skaggs Professor of Chemical Biology, Chairman of the Department of Chemistry at TSRI, and Professor of Chemistry at University of California, San Diego, describes the first solid-phase synthesis of epothilone A, the total synthesis of epothilone B and the generation of a library of epothilones that could be screened for potentially useful pharmaceutical compounds.

According to Nicolaou, "The importance of total chemical synthesis of compounds such as the epothilones lies in our ability to create analogs of the naturally occurring compounds that could ultimately provide additional therapeutic benefits without damaging side effects."

Epothilones A and B are produced naturally by the myxobacterium Sorangium cellulosum. Like Taxol , they exhibit cytotoxicity in cancer cells by interfering with their ability to divide and replicate. This is accomplished by their interaction with and stabilization of those sections of the cell known as microtubules, or the microscopic skeletons of the cells.

While the mechanism of inhibition appears to be similar in Taxol and epothilone, Nicolaou's work demonstrates the latter's ability to destroy tumor cells even in Taxol -resistant cell lines.

According to Nicolaou, solid-phase synthesis applied here to epothilone A, "could open up new possibilities in natural-product synthesis and, together with solution-phase synthesis of other epothilones, paves the way for the generation of large combinatorial libraries of these important molecules for biological screening."

Funding for the study was provided by the National Institutes of Health, Skaggs Institute for Chemical Biology, CaPCURE, and biotechnology and pharmaceutical companies.


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