Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.

Harish Rajak, Pramod Kumar, Poonam Parmar, Bhupendra Singh Thakur, Ravichandran Veerasamy, Prabodh Chander Sharma, Ajay Kumar Sharma, Arun Kumar Gupta, Jawahar Singh Dangi

Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur 495 009, CG, India. harishdops@yahoo.co.in

European journal of medicinal chemistry 2012 Jul

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Histone deacetylase inhibitors have been actively explored as a new generation of chemotherapeutics for cancers, generally known as epigenetic therapeutics. Two novel series of N-(2-amino-phenyl)-4-{[(2/3/4-substituted-phenylcarbamoyl)-methyl]-amino}-butyramide and N-(2-amino-phenyl)-4-{[(2/3/4-substituted-phenylcarbamoyl)-methyl]-amino}benzamide were designed and synthesized as novel histone deacetylase inhibitors. The anticancer potential of the compounds were determined in-vitro using MTT assay against HCT-116 and U251 (glioma) cell lines and histone deacetylase inhibitory assay. The synthesized compounds were investigated for anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells in Swiss albino mice. The efforts were also made to ascertain structure-activity relationships among test compounds. The results of the present studying represents appraisal of γ-aminobutyric acid (GABA) and para-aminobenzoic acid (PABA) as linker moiety for development of newer benzamide based histone deacetylase inhibitor. Copyright © 2012 Elsevier Masson SAS. All rights reserved.

Citation

Harish Rajak, Pramod Kumar, Poonam Parmar, Bhupendra Singh Thakur, Ravichandran Veerasamy, Prabodh Chander Sharma, Ajay Kumar Sharma, Arun Kumar Gupta, Jawahar Singh Dangi. Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. European journal of medicinal chemistry. 2012 Jul;53:390-7