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

Molecules

Aisha R. Al-Marhabi²  Hebat-Allah S. Abbas¹  Yousry A. Ammar³ 

[1] Department of Chemistry, Faculty of Science, King Khalid University, Abha 9004, Saudi ArabiaDepartment of Chemistry, University College in Qunfudah, Umm Al Qura University, Qunfudah 21955, Saudi Arabia;Department of Chemistry, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt;

关键词: quinoxaline;    tetrazoloquinoxaline;    1;    2;    4-triazoloquinoxaline;    1;    2;    4-triazino-quinoxaline;    anticancer agents;    antimicrobial agents;   

DOI  :  10.3390/molecules201119655

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.