Abstract
Cinnamoly compounds 1a-c and 2a-d were designed, synthesized, and in vitro tested as p300 inhibitors. At different degrees, all tested compounds were proven to inactivate p300, particularly, derivative 2c was the most active inhibitor, also showing high specificity for p300 as compared to other histone acetyltransferases. Most notably, 2c showed anti-acetylase activity in mammalian cells. These compounds represent a new class of synthetic inhibitors of p300, characterized by simple chemical structures.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Acetylation
-
Benzylidene Compounds / chemical synthesis*
-
Benzylidene Compounds / pharmacology
-
Cell Cycle Proteins / antagonists & inhibitors*
-
Cell Membrane Permeability
-
Cinnamates / chemical synthesis*
-
Cinnamates / pharmacology
-
Curcumin / analogs & derivatives
-
Curcumin / chemical synthesis
-
Curcumin / pharmacology
-
Cyclohexanones / chemical synthesis*
-
Cyclohexanones / pharmacology
-
HeLa Cells
-
Histone Acetyltransferases / antagonists & inhibitors*
-
Histones / metabolism
-
Humans
-
Recombinant Proteins / antagonists & inhibitors
-
Transcription Factors / antagonists & inhibitors*
-
p300-CBP Transcription Factors
Substances
-
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
-
Benzylidene Compounds
-
Cell Cycle Proteins
-
Cinnamates
-
Cyclohexanones
-
Histones
-
Recombinant Proteins
-
Transcription Factors
-
Histone Acetyltransferases
-
p300-CBP Transcription Factors
-
p300-CBP-associated factor
-
Curcumin