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

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 th...

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Bibliographic Details
Published in:	Chemical communications (Cambridge, England) no. 4; p. 462
Main Authors:	Paterson, Ian, Aceña, Jose L, Bach, Jordi, Chen, David Y K, Coster, Mark J
Format:	Journal Article
Language:	English
Published:	England 21-02-2003
Subjects:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Cell Division - drug effects Drug Resistance, Neoplasm Ethers, Cyclic - chemical synthesis Ethers, Cyclic - pharmacology Humans Lactones Macrolides - chemical synthesis Macrolides - pharmacology Paclitaxel Structure-Activity Relationship Tumor Cells, Cultured
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Summary:	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.
ISSN:	1359-7345
DOI:	10.1039/b212651f