Synthesis, Characterization and in silico evaluations of Diethyl-3-Methyl-5-(6-Methyl-2-Oxo-4-Phenyl- 1, 2, 3, 4-Tetrahydropyrimidine-5-Carboxamido) Thiophene-2, 4- Dicarboxylate Analogues as Anti-Proliferative and Anti-Microbial Agents

Author : Kalpesh Malani, Sampark S. Thakkar, Mukund Chandra Thakur, Pinakin Dhandhukia, Hiren V. Doshi

With an aim to develop potent anticancer agents, a series of diethyl-3-methyl-5-(6-methyl-2-oxo -4-phenyl-1, 2, 3, 4-tetrahydropyrimidine-5-carboxamido) thiophene-2, 4-dicarboxylate analogues (KM1-9) have been synthesized by conventional method and characterized by IR, Mass, NMR and elemental analysis. In silico studies have been done for all molecules (KM1-9) on Human topoisomerase IIbeta (PDB Id: 3QX3). The compounds were tested for in vitro antiproliferative activity on VERO and 786-O cell lines. The compound KM5 showed moderate activity on both cell lines. In vitro antimicrobial activity was checked against Bacillus Subtilis (BS), Staphylococcus Aurous (SA), Pseudomonas Aeruginosa (PA), Escherichia Coli (EC) and Candida Albicans (CA) by well diffusion method. The compounds KM3 and KM8 were found to have highest zone of inhibition against BS, SA, PA and EC. The Molecules KM8 and KM9 exhibited comparable activity against PA. The antifungal activity of all the analogous indicated weak activity against CA.

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