Design, synthesis and activity evaluation of indole-based double – Branched HDAC1 inhibitors

Bioorganic & Medicinal Chemistry
2019.0

Abstract

Histone deacetylases inhibitors (HDACIs) represents effective treatments for cancer. In continuing our efforts to develop novel and potent HDACIs, a series of N-hydroxycinnamamide-based HDACIs with aromatic ring and various aliphatic linker have been successfully designed and synthesized. Biological evaluations established that compounds 4h, 4i, 4j, 4l, 4r showed superior inhibition on histone deacetylase and antiproliferative activity in some solid tumor cell lines [HeLa, SK-N-BE(2), PC-3] compared to the known inhibitor SAHA. Among these analogs, 4l exhibited selectivity to HDAC1.

Knowledge Graph

Similar Paper

Design, synthesis and activity evaluation of indole-based double – Branched HDAC1 inhibitors
Bioorganic & Medicinal Chemistry 2019.0
Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with an Indole-Containing Cap Group
ACS Medicinal Chemistry Letters 2013.0
Development of N -hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity
Bioorganic & Medicinal Chemistry 2017.0
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2016.0
Synthesis and Biological Evaluation of 1-Arylsulfonyl-5-(N-hydroxyacrylamide)indoles as Potent Histone Deacetylase Inhibitors with Antitumor Activity in Vivo
Journal of Medicinal Chemistry 2012.0
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 di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2013.0
The design, synthesis and structure–activity relationships of novel isoindoline-based histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2011.0
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
European Journal of Medicinal Chemistry 2009.0
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
Bioorganic & Medicinal Chemistry 2015.0