Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
Bioorg Med Chem Lett
; 23(11): 3200-3, 2013 Jun 01.
Article
in En
| MEDLINE
| ID: mdl-23639537
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thiazoles
/
Drug Design
/
Histone Deacetylase Inhibitors
/
Heterocyclic Compounds, 3-Ring
/
Histone Deacetylases
/
Hydroxamic Acids
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2013
Type:
Article
Affiliation country:
China