Synthesis and biological evaluation of spongistatin/altohyrtin analogues: E-ring dehydration and C46 side-chain truncation |
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Authors: | Paterson Ian Aceña Jose L Bach Jordi Chen David Y K Coster Mark J |
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Institution: | University Chemical Laboratory, Lensfield Road, Cambridge, UK CB2 1EW. ip100@cam.ac.uk |
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Abstract: | Simplified analogues of the potent antimitotic marine macrolide spongistatin 1/altohyrtin A were synthesised and evaluated as growth inhibitory agents against a range of human tumour cell lines, including Taxol-resistant strains, revealing that E-ring dehydration leads to enhanced cytotoxicity at the low picomolar level while truncation of the side-chain at C46 results in a drastic decrease in activity. |
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