Synthesis and Pharmacological Evaluation of Pyrazole Substituted Coumarin Erivatives as Antibacterial/Anticancer Agents

Abstract

A series of novel 3-(4-substituted phenyl)-1-phenyl-1H-pyrazole-4- carbaldehyde containing 4-hydroxy-2H-chromen-2-one and 4- methyl-2-oxo-2H-chromen-7-yl acetate derivatives were synthesised via multicomponent reaction. Telomerase selected as target for anticancer activity. In normal condition it maintains chromosomal integrity and remains dormant but in cancer cell, telomerase get reactivated and maintain short length of telomeres and immortality. The essential role of telomerase in cancer and aging makes it an important target for the development of therapies to treat cancer. The structures of synthesised compound were elucidated by FTIR, Mass, 1H NMR and 13C NMR spectral analysis. For evaluation of anticancer activity synthesised compound were evaluated against NCIH-522 (Lung cancer) cell line. Doxorubicin selected as standard. From the investigation it was found that TJaf- 03 shows good cytotoxicity. While compound TJad-01 shows lowest activity on cell lines in comparison to other cell lines. Antibacterial activity of synthesized compounds was evaluated against Grampositive bacteria i.e. Staphylococcus aureus (MTCC-737) and Gramnegative bacteria i.e. Escherichia coli (MTCC-1687) by Disc Diffusion Method. Tjaf-03 showed good antibacterial activity against gram negative and positive strain in comparison with gentamycin and Vancomycin respectively.