Novel Pyrazolines: Synthesis and Evaluation of Their Derivatives with Anticancer and Anti-inflammatory Activities

Objective: Synthesis of novel pyrazolines (P2-P4 & P7-P9) from the chalcones (C2-C10) obtained by condensing different aldehydes with 2-acetyl5-bromothiophene and evaluates them for in vitro anticancer and anti-inflammatory activities. Methods: The synthesized pyrazolines and chalcones were screened for anticancer activity against human breast cancer cell lines-MCF-7 and MDAMB-468 in the range of 100 nm to 100 μm. Inhibition of bovine albumin denaturation and heat-induced hemolysis in vitro methods were followed to screen for anti-inflammatory activity. The structures of synthesized compounds were confirmed based on the IR, 1H NMR and mass spectral data. Results: Among the synthesized compounds, methoxy trisubstituted pyrazoline derivative (P6) exhibited an interesting profile of anticancer activity against MCF-7 cell line with GI50<0.1 μ M. similar to that of the standard drug doxorubicin. Compounds C8, P8, P3 have moderate antiinflammatory activity in bovine denaturation and heat induced hemolytic method. Conclusion: Novel pyrazolines and chalcones were synthesized and evaluated for anticancer and anti-inflammatory activity. The methoxy containing compounds one of which P6 found to be active against MCF-7 breast cancer cell line. The chloro-substituted compounds found to show anti-inflammatory activity.