Synthesis and biological evaluation of spongistatin/altohyrtin analogues: E-ring dehydration and C46 side-chain truncation

Literature Information

Publication Date 2003-01-23
DOI 10.1039/B212651F
Impact Factor 6.222
Authors

Ian Paterson, Jose L. Aceña, Jordi Bach, David Y.-K. Chen, Mark J. Coster


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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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