Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail.
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.
Hayat
Faisal
F
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Salahuddin
Attar
A
Umar
Sadiq
S
Azam
Amir
A
D000563:Amebicides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004748:Entamoeba histolytica / Q000187:drug effects*; D004749:Entamoebiasis / Q000188:drug therapy; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000563:Amebicides; D011720:Pyrazoles; D011804:Quinolines; C037219:quinoline