Issue 4, 2003

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

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.

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

Supplementary files

Article information

Article type
Communication
Submitted
23 Dec 2002
Accepted
15 Jan 2003
First published
23 Jan 2003

Chem. Commun., 2003, 462-463

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

I. Paterson, J. L. Aceña, J. Bach, D. Y.-K. Chen and M. J. Coster, Chem. Commun., 2003, 462 DOI: 10.1039/B212651F

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