Molecular Docking, Synthesis and Evaluation of Novel Hydroximic Acid Mimics as Anti-cancerous Histone Deacetylase Inhibitors
Journal Title: UNKNOWN - Year 2018, Vol 8, Issue 6
Abstract
In the current study, development of novel hydroximate mimics for HDAC-8 inhibition, as an anticancer target was carried out. To design the novel hydroximate, we must find out which protein can be targeted in pathogenesis so that, molecular docking was carried out and human HDAC-8 was found to be a potential cancer drug target for hydroximates. Focusing on identifying a potential HDAC-8 inhibitor, the Ligand-1 (IUPAC name: (N1 (2-hydroxyethyl) N8-phenyloctanediamide) has been identified as a potential and novel lead molecule further, the Ligand-1 was synthesized and characterized followed by cytotoxicity study against the MG-63 cell lines, in vitroHDAC enzyme inhibition assay and in vivo EAC model was carried out. The acute toxicity study (OECD-425) for LD50 was found to be 550 mg/kg/i.p and from this the final dose selected was 1/10th of 550 mg/kg that is 55 mg/kg, by using this dose in vivo was carried out with haematological parameters such as Hgb, RBCs, WBCs, %ILS, Body weight analysis and it was observed that Ligand-1 is extremely significant (P<0.05), from these results we concluded that, the novel hydroximic acid mimic that is Ligand-1 elicited as a remarkable anti-cancer activity.
Authors and Affiliations
Rajaganapathy Kaliyaperumal, Yogesh B Biradar, Manjunatha P Mudugal
Keywords
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