Synthesis and biological evaluation of 10,11-dihydrodictyostatin, a potent analogue of the marine anticancer agent dictyostatin

[摘要]：By employing a diverted total synthesis strategy with late-stage intermediates, 10,1 1-dihydrodictyostatin (5) was prepared and evaluated in vitro for growth inhibition against a range.of human cancer cell lines, including the NCI/ADR Taxolresistant 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.

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