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Abstract
The tenovins and cambinol are two classes of sirtuin inhibitor that exhibit antitumor activity in preclinical models. This report describes modifications to the core structure of cambinol, in particular by incorporation of substitutents at the N1-position, which lead to increased potency and modified selectivity. These improvements have been rationalized using molecular modeling techniques. The expected functional selectivity in cells was also observed for both a SIRT1 and a SIRT2 selective analog.
Original language | English |
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Pages (from-to) | 2673-2682 |
Number of pages | 10 |
Journal | Journal of Medicinal Chemistry |
Volume | 52 |
Issue number | 9 |
Early online date | 1 Apr 2009 |
DOIs | |
Publication status | Published - 14 May 2009 |
Keywords
- Small-Molecule Inhibitor
- P53
- SIR2
- Deacetylase
- Binding
- Survival
- Homolog
- Disease
- Enzymes
- Mice
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Dive into the research topics of 'Novel Cambinol analogs as Sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity'. Together they form a unique fingerprint.Projects
- 1 Finished
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ROYAL SOCIETY RESEARCH FELLOWSHIP: Chemical Genetic Approach
Westwood, N. J. (PI)
1/10/01 → 30/09/09
Project: Fellowship