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

2010; Elsevier BV; Volume: 45; Issue: 10 Linguagem: Inglês

10.1016/j.ejmech.2010.07.028

1768-3254

Faisal Hayat, Salahuddin Attar, Sadiq Umar, Amir Azam,

Cancer therapeutics and mechanisms

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 (IC50 = 0.05 μM, 0.31 μM, 0.06 μM, 0.29 μM) respectively than the standard drug metronidazole (IC50 = 1.84 μM). 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 μM.