Synthesis and biological evaluation of spongistatin/altohyrtin analogues: E-Ring dehydration and C46 side-chain truncation
Author(s)
Paterson, I
Acena, JL
Bach, J
Chen, DYK
Coster, MJ
Griffith University Author(s)
Year published
2003
Metadata
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Simplified analogs of the potent antimitotic marine macrolide spongistatin 1/altohyrtin A were synthesized and evaluated as growth inhibitory agents against a range of human tumor 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.Simplified analogs of the potent antimitotic marine macrolide spongistatin 1/altohyrtin A were synthesized and evaluated as growth inhibitory agents against a range of human tumor 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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Journal Title
Chemical Communications
Volume
2003
Publisher URI
Subject
Chemical sciences