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  • Title: Total synthesis and biological evaluation of potent analogues of dictyostatin: modification of the C2-C6 dienoate region.
    Author: Paterson I, Gardner NM, Guzmán E, Wright AE.
    Journal: Bioorg Med Chem Lett; 2008 Dec 01; 18(23):6268-72. PubMed ID: 18951787.
    Abstract:
    By exploiting a Still-Gennari olefination of a common C11-C26 aldehyde with a C4-C10 or C1-C10 beta-ketophosphonate, three modified C2-C6 region analogues of the 22-membered macrolide dictyostatin were synthesised and evaluated in vitro for growth inhibition against a range of human cancer cell lines, including the Taxol-resistant NCI/ADR-Res cell line. 6-Desmethyldictyostatin and 2,3-dihydrodictyostatin displayed potent (low nanomolar) antiproliferative activity, intermediate between dictyostatin and discodermolide, while 2,3,4,5-tetrahydrodictyostatin showed activity comparable to discodermolide. As with dictyostatin, these simplified analogues act through a mechanism of microtubule stabilisation, G2/M arrest and apoptosis.
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