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.
Authors	Ian Paterson, Jose L Aceña, Jordi Bach, David Y K Chen, Mark J Coster
Journal	Chemical communications (Cambridge, England) (Chem Commun (Camb)) Issue 4 Pg. 462-3 (Feb 21 2003) ISSN: 1359-7345 [Print] England
PMID	12638950 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antineoplastic Agents Ethers, Cyclic Lactones Macrolides spongistatin 1 Paclitaxel
Topics	Antineoplastic Agents (chemical synthesis, pharmacology) Cell Division (drug effects) Drug Resistance, Neoplasm Ethers, Cyclic (chemical synthesis, pharmacology) Humans Lactones Macrolides (chemical synthesis, pharmacology) Paclitaxel Structure-Activity Relationship Tumor Cells, Cultured

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