1005176-29-3Relevant academic research and scientific papers
Total synthesis of (-)-dictyostatin, a microtubule-stabilising anticancer macrolide of marine sponge origin
Paterson, Ian,Britton, Robert,Delgado, Oscar,Gardner, Nicola M.,Meyer, Arndt,Naylor, Guy J.,Poullennec, Karine G.
scheme or table, p. 6534 - 6545 (2010/10/03)
An efficient convergent synthesis of the anticancer marine macrolide (-)-dictyostatin is described that proceeds in 4.6% yield over 27 steps. Most of the stereocentres were configured using substrate control, making use of a common building block to insta
Synthesis and biological evaluation of 10,11-dihydrodictyostatin, a potent analogue of the marine anticancer agent dictyostatin
Paterson, Ian,Gardner, Nicola M.,Poullennec, Karine G.,Wright, Amy E.
experimental part, p. 364 - 369 (2009/04/11)
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.
