Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail

  • Eur J Med Chem. 2010 Oct;45(10):4669-75. doi: 10.1016/j.ejmech.2010.07.028.
Faisal Hayat  1 ,  Attar Salahuddin ,  Sadiq Umar ,  Amir Azam
Affiliations
  • 1. Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
PMID: 20696501 DOI: 10.1016/j.ejmech.2010.07.028
Abstract

The cyclization of Chalcones (1a-1j) with 2-(quinolin-8-yloxy) acetohydrazide (2) under basic condition led to the formation of new compounds, pyrazoline derivatives (3a-3j). In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that the compounds 3d, 3g, 3h, and 3j exhibited promising antiamoebic activity (IC(50) = 0.05 microM, 0.31 microM, 0.06 microM, 0.29 microM) respectively than the standard drug metronidazole (IC(50) = 1.84 microM). The toxicological studies of these compounds on human breast Cancer MCF-7 cell line showed that all the compounds 3d, 3g, 3h, 3j and metronidazole were nontoxic at the concentration range of 1.56-50 microM.