Literature

Abstract

Inhibition of HDACs activity has become a promising therapeutic strategy in clinical practice to reverse the abnormal epigenetic states of cancer and other diseases. Therefore, HDAC inhibitors become a relatively new class of anti-cancer agent. In the present study, we reported the design and synthesis of a series of novel HDAC inhibitors using various substituted quinoline rings as the cap group. In vitro studies showed that some compounds have good inhibitory activities against HDACs and potent antiproliferative activities in some tumor cell lines. Especially, compound 9w (IC50=85 nM), exhibited better inhibitory effect compared with SAHA (IC50=161 nM).

DOI： 10.1016/j.bmc.2015.06.024

Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

Bioorganic & Medicinal Chemistry 2015.0

Design, synthesis and bioactivity evaluations of 8-substituted-quinoline-2-carboxamide derivatives as novel histone deacetylase (HDAC) inhibitors

Bioorganic & Medicinal Chemistry 2023.0

Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry 2016.0

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 novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups

Bioorganic & Medicinal Chemistry Letters 2017.0

Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors