NOVEL PYRAZOLINES: SYNTHESIS AND EVALUATION OF THEIR DERIVATIVES WITH ANTICANCER AND ANTI-INFLAMMATORY ACTIVITIES

  • L. Siva Sanker Reddy Dept. of Pharmaceutical Chemistry, Creative Educational Society’s College of Pharmacy, N. H-7, Chinnatekur, Kurnool, Andhra Pradesh 518218
  • M. Bhagavan Raju Gland Institute of Pharmaceutical Sciences,
  • C. Sridhar Sri Padmavathi School of Pharmaceutical Sciences

Abstract

Objective: Synthesis of novel pyrazolines (P2-P4 & P7-P9) from the chalcones (C2-C10) obtained by condensing different aldehydes with 2-acetyl- 5-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 MDA-MB-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 anti-inflammatory 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.

 

Keywords: Pyrazoline, Chalcone, MCF-7, MDA-MB-468, Anti-inflammatory, Anticancer

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How to Cite
Reddy, L. S. S., M. B. Raju, and C. Sridhar. “NOVEL PYRAZOLINES: SYNTHESIS AND EVALUATION OF THEIR DERIVATIVES WITH ANTICANCER AND ANTI-INFLAMMATORY ACTIVITIES”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 8, no. 1, Nov. 2015, pp. 247-54, https://innovareacademics.in/journals/index.php/ijpps/article/view/7707.
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