Page 34 - I. Chemical biology and drug discovery
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[I. Chemical biology and drug discovery-18]
Synthesis of novel fluoro- and biary-benzamide based
histone deacetylase inhibitors and their biological evaluation
Minh Thanh La¹, Hee-Kwon Kim¹˙*
¹Department of Nuclear Medicine, Jeonbuk National University , Jeonju 54907, Republic of Korea
In was commonly known that Histone deacetylases (HDACs) influence gene expression regulation and cell state.
Inhibition of histone deacetylases was related with a variety of biological phenomena such as growth cell
differentiation, growth arrest, regulation of metabolism, or apoptosis of tumor cell lines. Due to their play in
biological system, various study for HDACs have been carried out to develop the promising bioactive agents.
Benzamide structure is one of useful crucial moiety to find promising HDAC inhibitors because some FDA approved
anticancer drugs such as Entinostat bears benzamide moiety. Herein, we designed novel type of fluoro and biaryl
benzamide based HDAC inhibitors which contain the cap group and zinc binding domain group. And then the
biological evaluation of newly prepared HDAC inhibitors were performed to see HDAC inhibitory activities.
