Synthesis of novel discodermolide analogues with modified hydrogen-bonding donor/acceptor sites |
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Authors: | Ian PatersonOscar Delgado |
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Institution: | University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, UK |
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Abstract: | A series of novel structural analogues of the potent microtubule-stabilizing anticancer agent discodermolide were synthesised, with modifications in the C16-C20 region to create new oxygenated H-bonding donor/acceptor sites for tubulin binding. By starting from an advanced C9-C24 intermediate, fully synthetic discodermolide analogues, incorporating either an additional hydroxyl group 3, an oxetane 4 or a cyclic carbonate 5, were obtained in 10 or 11 steps by using a versatile aldol construction of the C6-C7 bond. |
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