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

• Main Authors: Aisha R. Al-Marhabi, Hebat-Allah S. Abbas, Yousry A. Ammar
• Format: Article
• Language: English
• Published: MDPI AG 2015-11-01
• Series: Molecules
• Subjects: quinoxaline; tetrazoloquinoxaline; 1,2,4-triazoloquinoxaline; 1,2,4-triazino-quinoxaline; anticancer agents; antimicrobial agents
• Online Access: http://www.mdpi.com/1420-3049/20/11/19655

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.