Literature DB >> 20696501

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

Faisal Hayat1, Attar Salahuddin, Sadiq Umar, Amir Azam.   

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.
Copyright © 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 20696501     DOI: 10.1016/j.ejmech.2010.07.028

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  7 in total

1.  One Pot Synthesis, Photophysical and X-ray Studies of Novel Highly Fluorescent Isoquinoline Derivatives with Higher Antibacterial Efficacy Based on the In-vitro and Density Functional Theory.

Authors:  Abdullah M Asiri; Salman A Khan; Saad H Al-Thaqafy; Kamlesh Sharma
Journal:  J Fluoresc       Date:  2015-03-05       Impact factor: 2.217

2.  Pyrazolo[3,4-d]pyrimidines as novel inhibitors of O-acetyl-L-serine sulfhydrylase of Entamoeba histolytica: an in silico study.

Authors:  Umesh Yadava; Bindesh Kumar Shukla; Mihir Roychoudhury; Devesh Kumar
Journal:  J Mol Model       Date:  2015-03-25       Impact factor: 1.810

3.  Design and Synthesis of Carbothioamide/Carboxamide-Based Pyrazoline Analogs as Potential Anticancer Agents: Apoptosis, Molecular Docking, ADME Assay, and DNA Binding Studies.

Authors:  Manish Rana; Md Imam Faizan; Sajad Hussain Dar; Tanveer Ahmad
Journal:  ACS Omega       Date:  2022-06-23

4.  Synthesis of some dihydropyrimidine-based compounds bearing pyrazoline moiety and evaluation of their antiproliferative activity.

Authors:  Fadi M Awadallah; Gary A Piazza; Bernard D Gary; Adam B Keeton; Joshua C Canzoneri
Journal:  Eur J Med Chem       Date:  2013-10-09       Impact factor: 6.514

5.  Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease.

Authors:  Oya Unsal-Tan; Tuba Tüylü Küçükkılınç; Beyza Ayazgök; Ayla Balkan; Keriman Ozadali-Sari
Journal:  Medchemcomm       Date:  2019-05-09       Impact factor: 3.597

Review 6.  Recent advances in the therapeutic applications of pyrazolines.

Authors:  Mohamed R Shaaban; Abdelrahman S Mayhoub; Ahmad M Farag
Journal:  Expert Opin Ther Pat       Date:  2012-03-08       Impact factor: 6.674

7.  Reaction of 7α-bromo-6-nitrocholest-5-enes with hydrazine: Formation of steroidal pyrazolines and molecular docking against SARS-CoV-2 omicron protease.

Authors:  Avadhesh Kumar; Mehtab Parveen; Mahboob Alam
Journal:  Steroids       Date:  2022-10-05       Impact factor: 2.760

  7 in total

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