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Updated: Sep 26, 2026
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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of spongistatin/altohyrtin analogues: E-ring dehydration and C46 side-chain
Ian Paterson1, Jose L Aceña, Jordi Bach
1University Chemical Laboratory, Lensfield Road, Cambridge, UK CB2 1EW. ip100@cam.ac.uk
Chemical Communications (Cambridge, England)
|March 18, 2003
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.
