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

Faisal Hayat, Attar Salahuddin, Sadiq Umar, Amir Azam

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79 Scopus citations

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 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.

Original languageEnglish (US)
Pages (from-to)4669-4675
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume45
Issue number10
DOIs
StatePublished - Oct 2010

Bibliographical note

Funding Information:
This work was supported by Council of Scientific and Industrial Research (grant # 01(2278)/08/EMR-II New Delhi, India). One of us (F.H) is thankful to the University Grant commission (UGC), India for the financial support.

Keywords

  • Entamoeba histolytica
  • MTT assay
  • Pyrazoline derivatives

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