Discovery of 4-methyl-2-oxo-2H-chromen-7-yl-2-benzamidoacetate as Anti-proliferative Agents
Journal Title: International Journal of Ayurveda and Pharmaceutical Chemistry - Year 2018, Vol 0, Issue 0
Abstract
Coumarin scaffolds are well known for exhibiting tremendous anti-tumor activity. The present work involved synthesis of a coumarin hybrid utilizing hippuric acid and screening of its antineoplastic potential. The coumarin scaffold (3) was fabricated utilizing the PechmanCondensation method. In this method, the phenolic derivative (1) and 3-keto esters (2) were made to react in the presence of a Lewis acid catalyst (Conc. H2SO4). To facilitate substitution at the 7th position of the coumarin scaffold, the hydroxyl group was replaced by the chloride function utilizing POCl3. In the ultimate step, hippuric acid (5) was made to react in the presence of conc. HCl to form hippuric acid-coumarin hybrid (6). The in vitro anti-cancer screening was performed against breast cancer cell line MCF-7 employing Sulforhodamine B (SRB) assay. The study represented the synthesis of coumarin hybrid utilizing hippuric acid. The spectroscopic, physicochemical, and elemental analyses data were found to be quite complimentary to the proposed structures. The compound showed a very promising anti-cancer activity (IC50 value of 31.88 μM) as compared to the marketed drug capecitabine (IC50 value of 6.87 μM). The study will surely endorse investigators across the globe in designing more analogs with pronounced activities in coming future
Authors and Affiliations
Chitralekha Deorao Padole, Mrunali Digambar Amdare, Kamna Rajesh Jogdand, Latika Liladhar Kathane, Nutan Ganesh Kuhite, Debarshi Kar Mahapatra
Keywords
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