Issue 46, 2014
From the journal:

RSC Advances

Synthesis and biological evaluation of some new triazolo[1,5-a]quinoline derivatives as anticancer and antimicrobial agents

Fatma A Bassyouni,*a   Sherifa M. Abu-Baker,b   Khaled Mahmoud,c   Maysa Moharam,d   Sally S. El-Nakkadyb  and  Mohamed Abdel Rehime  

* Corresponding authors

a Chemistry of Natural and Microbial Products Department, Pharmaceutical Research Group, Center of Excellence for Advanced Sciences, National Research Centre, Cairo, Egypt
E-mail: fatma.nrc@hotmail.com
Fax: +20-233370931
Tel: +20-1118596967

b Chemistry Department of Natural and Microbial Products, National Research Centre, Cairo, Egypt

c Pharmacognosy Department, National Research Centre, Cairo, Egypt

d Chemistry Department of Microbial Products, National Research Centre, Cairo, Egypt

e Department of Analytical Chemistry, Stockholm University, 10691 Stockholm, Sweden

Abstract

In the present study, versatile multifunctional unreported triazolo[1,5-a]quinoline derivatives were prepared. Compounds 1–19 were synthesized by adopting appropriate synthetic routes and were pharmacologically evaluated for their in vitro anticancer activity against human cancer cell lines: hepatocellular liver carcinoma (HEPG2) and Caucasian breast adenocarcinoma (MCF-7), in addition to their antibacterial and antifungal activities. Compound 4 demonstrated strong inhibitory effects against breast cancer (MCF-7), whereas compounds 8 and 19 exhibited moderate activity against breast carcinoma cell line MCF-7. Compounds 16 and 19 gave moderate activity against liver carcinoma cell line HEPG2. The antimicrobial activity of the prepared compounds was tested against bacteria and fungi. Among them, the results of antimicrobial activity indicated that compounds 4, 9, 11, 13, 15, 17, 18 and 19 were the most active compounds. Compound 4 exhibited strong activity against Fusarium sp., whereas compounds 9, 11, 15, 17, 18 and 19 showed high activity against Escherichia coli. More specifically, compound 17 displayed a high inhibitory effect against Bacillus cereus, Escherichia coli and Rhizoctonia sp.

Graphical abstract: Synthesis and biological evaluation of some new triazolo[1,5-a]quinoline derivatives as anticancer and antimicrobial agents

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Article information

DOI
https://doi.org/10.1039/C3RA46961A
Article type
Paper
Submitted
22 Nov 2013
Accepted
07 Apr 2014
First published
09 Jun 2014

RSC Adv., 2014,4, 24131-24141

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Synthesis and biological evaluation of some new triazolo[1,5-a]quinoline derivatives as anticancer and antimicrobial agents

F. A Bassyouni, S. M. Abu-Baker, K. Mahmoud, M. Moharam, S. S. El-Nakkady and M. A. Rehim, RSC Adv., 2014, 4, 24131 DOI: 10.1039/C3RA46961A

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