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Molecules 2015, 20(11), 19805-19822; doi:10.3390/molecules201119655

Synthesis, Characterization and Biological Evaluation of Some Quinoxaline Derivatives: A Promising and Potent New Class of Antitumor and Antimicrobial Agents

1
Department of Chemistry, University College in Qunfudah, Umm Al Qura University, Qunfudah 21955, Saudi Arabia
2
Department of Chemistry, Faculty of Science, King Khalid University, Abha 9004, Saudi Arabia
3
Department of Photochemistry, National Research Centre, Dokki 12622, Egypt
4
Department of Chemistry, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 13 August 2015 / Revised: 22 October 2015 / Accepted: 26 October 2015 / Published: 3 November 2015
(This article belongs to the Section Bioorganic Chemistry)
View Full-Text   |   Download PDF [841 KB, uploaded 3 November 2015]   |  

Abstract

In continuation of our endeavor towards the development of potent and effective anticancer and antimicrobial agents; the present work deals with the synthesis of some novel tetrazolo[1,5-a]quinoxalines, N-pyrazoloquinoxalines, the corresponding Schiff bases, 1,2,4-triazinoquinoxalines and 1,2,4-triazoloquinoxalines. These compounds were synthesized via the reaction of the key intermediate hydrazinoquinoxalines with various reagents and evaluated for anticancer and antimicrobial activity. The results indicated that tetrazolo[1,5-a]quinoxaline derivatives showed the best result, with the highest inhibitory effects towards the three tested tumor cell lines, which were higher than that of the reference doxorubicin and these compounds were non-cytotoxic to normal cells (IC50 values > 100 μg/mL). Also, most of synthesized compounds exhibited the highest degrees of inhibition against the tested strains of Gram positive and negative bacteria, so tetrazolo[1,5-a]quinoxaline derivatives show dual activity as anticancer and antimicrobial agents. View Full-Text
Keywords: quinoxaline; tetrazoloquinoxaline; 1,2,4-triazoloquinoxaline; 1,2,4-triazino-quinoxaline; anticancer agents; antimicrobial agents quinoxaline; tetrazoloquinoxaline; 1,2,4-triazoloquinoxaline; 1,2,4-triazino-quinoxaline; anticancer agents; antimicrobial agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Al-Marhabi, A.R.; Abbas, H.-A.S.; Ammar, Y.A. Synthesis, Characterization and Biological Evaluation of Some Quinoxaline Derivatives: A Promising and Potent New Class of Antitumor and Antimicrobial Agents. Molecules 2015, 20, 19805-19822.

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