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Open Access Natural Product-Based Drug Discovery – Epothilones as Lead Structures for the Discovery of New Anticancer Agents

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Epothilones are microtubule depolymerization inhibitors, which inhibit the growth of a broad range of human cancer cell lines in vitro with low nM or sub-nM IC50s. Unlike other cytotoxic anticancer agents, epothilones are also active in vitro against multidrug-resistant cell lines and they inhibit the growth of multidrug-resistant tumors in vivo. In order to further our understanding of the structural requirements for biological activity and, ultimately, to identify new microtubule-stabilizing agents with improved overall properties, we have investigated the biological activity of a variety of structurally modified epothilone analogs. This report will focus on two selected aspects of our SAR work, namely (1) the synthesis and biological characterization of a series of 12-aza epothilones and (2) analogs with a conformationally constrained side-chain. Several of these structures exhibit potent in vitro antiproliferative activity, and thus may be interesting candidates for further profiling in tumor models and perhaps for the development of improved clinical candidates.

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Keywords: ANTIPROLIFERATIVE ACTIVITY; ANTITUMOR ACTIVITY; EPOTHILONES; NATURAL PRODUCTS; STRUCTURE ACTIVITY RELATIONSHIPS

Document Type: Editorial

Publication date: October 1, 2004

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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