Cryptocaryol Structure–Activity Relationship Study of Cancer Cell Cytotoxicity and Ability to Stabilize PDCD4

The synthetic cryptocaryols A and B and a series of their analogues have been evaluated for their cytotoxicity and their ability to stabilize the tumor suppressor PDCD4. Cytotoxicities in the 3 to 30 μM range were found. Both the cytotoxicity and PDCD4 stabilizing ability were tolerant of large ster...

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Bibliographic Details
Published in:ACS medicinal chemistry letters Vol. 5; no. 5; pp. 522 - 526
Main Authors: Cuccarese, Michael F, Wang, Yanping, Beuning, Penny J, O’Doherty, George A
Format: Journal Article
Language:English
Published: United States American Chemical Society 08-05-2014
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Summary:The synthetic cryptocaryols A and B and a series of their analogues have been evaluated for their cytotoxicity and their ability to stabilize the tumor suppressor PDCD4. Cytotoxicities in the 3 to 30 μM range were found. Both the cytotoxicity and PDCD4 stabilizing ability were tolerant of large stereochemical changes to the molecule. Co-dosing studies with cryptocaryols A and B and several known cancer drugs showed no measuable enhancement in cancer drug cytotoxicity.
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ISSN:1948-5875
1948-5875
DOI:10.1021/ml4005039