Synthesis and Biological Evaluation of 10,11-Dihydrodictyostatin, a Potent Analogue of the Marine Anticancer Agent Dictyostatin

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• 作者：Ian Paterson ; Nicola M. Gardner ; Karine G. Poullennec ; Amy E. Wright
• 刊名：Journal of Natural Products
• 出版年：2008
• 出版时间：March 2008
• 年：2008
• 卷：71
• 期：3
• 页码：364 - 369
• 全文大小：655K
• 年卷期：v.71,no.3(March 2008)
• ISSN：1520-6025

文摘

By employing a diverted total synthesis strategy with late-stage intermediates, 10,11-dihydrodictyostatin (5) was prepared and evaluated in vitro for growth inhibition against a range of human cancer cell lines, including the NCI/ADR Taxol-resistant cell line. This novel dictyostatin analogue was found to retain potent antimitotic activity, with a comparable profile to discodermolide and Taxol, functioning by microtubule stabilization and G2/M arrest. These SAR studies provide further insight into the interaction between dictyostatin (1) and its tubulin target.