Design, synthesis and biological evaluation of bridged epothilone D analogues
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چکیده
منابع مشابه
Design, synthesis and biological evaluation of bridged epothilone D analogues.
Six epothilone D analogues with a bridge between the C4-methyl and the C12-methyl carbons were prepared in an attempt to constrain epothilone D to its proposed tubulin-binding conformation. Ring-closing metathesis (RCM) was employed as the key step to build the C4-C26 bridge. In antiproliferative assays in the human ovarian cancer (A2780) and prostate cancer (PC3) cell lines, and also in tubuli...
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The synthesis of two deoxygenated analogues of potent epothilones is reported in an effort to analyze the relative importance of molecular conformation and ligand-target interactions to biological activity. 7-deoxy-epothilone D and 7-deoxy-(S)-14-methoxy-epothilone D were prepared through total synthesis and shown to maintain the conformational preferences of their biologically active parent co...
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ژورنال
عنوان ژورنال: Organic & Biomolecular Chemistry
سال: 2008
ISSN: 1477-0520,1477-0539
DOI: 10.1039/b814823f