Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases

Bioorganic & Medicinal Chemistry Letters
2010.0

Abstract

Inhibition of histone deacetylase activity represents a promising new modality in the treatment of a number of cancers. A novel HDAC series demonstrating inhibitory activity in cell proliferation assays is described. Optimisation based on the introduction of basic amine linkers to effect good drug distribution to tumour led to the identification of a compound with oral activity in a human colon cancer xenograft study associated with increased histone H3 acetylation in tumour tissue.

Knowledge Graph

Similar Paper

Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases
Bioorganic & Medicinal Chemistry Letters 2010.0
Novel amide derivatives as inhibitors of histone deacetylase: Design, synthesis and SAR
European Journal of Medicinal Chemistry 2009.0
2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: Design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2011.0
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2016.0
Design and synthesis of a novel class of histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2001.0
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities
Bioorganic & Medicinal Chemistry Letters 2019.0
Antiproliferative and Differentiating Activities of a Novel Series of Histone Deacetylase Inhibitors
ACS Medicinal Chemistry Letters 2010.0
Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors
Bioorganic & Medicinal Chemistry 2011.0
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2014.0
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2014.0