The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar' is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alk
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Page/Page column 25
(2010/04/27)
Novel cambinol analogs as sirtuin inhibitors: Synthesis, biological evaluation, and rationalization of activity
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.
Medda, Federico,Russell, Rupert J. M.,Higgins, Maureen,McCarthy, Anna R.,Campbell, Johanna,Slawin, Alexandra M. Z.,Lane, David P.,Lain, Sonia,Westwood, Nicholas J.
experimental part
p. 2673 - 2682
(2010/01/16)
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