Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters
2013.0

Abstract

Novel indeno[1,2-d]thiazole hydroxamic acids were designed, synthesized, and evaluated for histone deacetylases (HDACs) inhibition and antiproliferative activities on tumor cell lines. Most of the tested compounds exhibited HDAC inhibition and antiproliferative activity against both MCF7 and HCT116 cells with GI50 values in the sub-micromolar range. Among them, compound 6o showed good inhibitory activity against pan-HDAC with IC50 value of 0.14 μM and significant growth inhibition on MCF7 and HCT116 cells with GI50 values of 0.869 and 0.535 μM, respectively.

Knowledge Graph

Similar Paper

Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2013.0
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
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 indole-based hydroxamic acid derivatives as histone deacetylase inhibitors
European Journal of Medicinal Chemistry 2022.0
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
The design, synthesis and structure–activity relationships of novel isoindoline-based histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2011.0
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors
Bioorganic & Medicinal Chemistry 2015.0
Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors
European Journal of Medicinal Chemistry 2017.0
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
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