Abstract: Novel 3-(4-aroyl-2-pyrrolyl)-N-hydroxy-2-propen-amides are disclosed as a new class of histone deacetylase (HDAC) inhibitors. Three-dimensional structure-based drug design and conformational analyses into the histone deacet-ylase-like protein (HDLP) catalytic core suggested the syn-thesis and biological evaluation of compounds 7a-h. Experi-mental pKi values are in good agreement with VALIDATE predicted pKi values of new derivatives. All compounds 7a-h show HDAC inhibitory activity in the micromolar range, with 7e as the most potent derivative (IC50) 1.9 íM). The influence of the 4′-substituent in the aroyl moiety is not significant for the inhibitory activity, as all compounds 7a-g show IC50 values between 1.9 and 3.9 íM. Otherwis...
International audienceInhibition of histone deacetylases (HDACs) leads to growth arrest, differentia...
We previously identified 3-hydroxypyridine-2-thione (3HPT) as a novel zinc binding group for histone...
Aim: Histone deacetylases (HDACs) regulate the expression and activity of numerous proteins involved...
Novel 3-(4-aroyl-2-pyrrolyl)-N-hydroxy-2-propenamides are disclosed as a new class of histone deacet...
Aroyl-pyrrole-hydroxy-amides (APHAs) are a new class of synthetic HDAC inhibitors recently described...
The binding mode of 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides 1a-c, belonging to a recently...
The binding mode of 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides 1a-c, belonging to a recentl...
The novel aroyl-pyrrolyl hydroxyamides 4a¿a¿ are analogues of the lead compound 3-(1-methyl-4-phenyl...
The novel aroyl-pyrrolyl hydroxyamides 4a-a are analogues of the lead compound 3-(1-methyl-4-phenyla...
A novel series of aroyl-pyrrolyl-hydroxy-amides (APHAs) active as histone deacetylase (HDAC) inhibit...
Previous SAR studies (Part 1: Mai, A.; et al. J. Med. Chem. 2003, 46, 512-524) performed on some por...
Aroyl-pyrrolyl-hydroxy-amides (APHAs) are a class of synthetic HDAC inhibitors described by us since...
Herein we describe the design, synthesis, and biological evaluation of new hydroxamic tertiary amine...
Wünsch M, Senger J, Schultheisz P, et al. Structure-Activity Relationship of Propargylamine-Based HD...
The novel aroyl-pyrrolyl hydroxyamides 4 a-a' are analogues of the lead compound 3-(1-methyl-4-phe...
International audienceInhibition of histone deacetylases (HDACs) leads to growth arrest, differentia...
We previously identified 3-hydroxypyridine-2-thione (3HPT) as a novel zinc binding group for histone...
Aim: Histone deacetylases (HDACs) regulate the expression and activity of numerous proteins involved...
Novel 3-(4-aroyl-2-pyrrolyl)-N-hydroxy-2-propenamides are disclosed as a new class of histone deacet...
Aroyl-pyrrole-hydroxy-amides (APHAs) are a new class of synthetic HDAC inhibitors recently described...
The binding mode of 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides 1a-c, belonging to a recently...
The binding mode of 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides 1a-c, belonging to a recentl...
The novel aroyl-pyrrolyl hydroxyamides 4a¿a¿ are analogues of the lead compound 3-(1-methyl-4-phenyl...
The novel aroyl-pyrrolyl hydroxyamides 4a-a are analogues of the lead compound 3-(1-methyl-4-phenyla...
A novel series of aroyl-pyrrolyl-hydroxy-amides (APHAs) active as histone deacetylase (HDAC) inhibit...
Previous SAR studies (Part 1: Mai, A.; et al. J. Med. Chem. 2003, 46, 512-524) performed on some por...
Aroyl-pyrrolyl-hydroxy-amides (APHAs) are a class of synthetic HDAC inhibitors described by us since...
Herein we describe the design, synthesis, and biological evaluation of new hydroxamic tertiary amine...
Wünsch M, Senger J, Schultheisz P, et al. Structure-Activity Relationship of Propargylamine-Based HD...
The novel aroyl-pyrrolyl hydroxyamides 4 a-a' are analogues of the lead compound 3-(1-methyl-4-phe...
International audienceInhibition of histone deacetylases (HDACs) leads to growth arrest, differentia...
We previously identified 3-hydroxypyridine-2-thione (3HPT) as a novel zinc binding group for histone...
Aim: Histone deacetylases (HDACs) regulate the expression and activity of numerous proteins involved...