Synthesis and biological evaluation of new 3-(4-substituted phenyl)aminoquinoxaline derivatives as anticancer agents

Heterocyclic communications

article

Mohamed G. Thabit¹  Serry A.A. El Bialy¹  Magda N.A. Nasr¹ 

[1] Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, Mansoura University

关键词: anticancer;    isoxazolines;    pyrazolines;    pyridines;    pyrimidines;    quinoxaline;   

DOI  :  10.1515/hc-2014-0081

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

Quinoxaline derivatives 4–11 were synthesized and evaluated for their in vitro growth inhibitory activities against liver carcinoma cell line (HEPG 2 ) using the sulforhodiamine B assay. The synthesis was achieved by reaction of 2,3-dichloroquinoxalines 2a,b with 4-aminoacetophenone to give the corresponding compounds 3a,b . Claisen-Schmidt condensation reaction of 3a,b with furfuraldehyde gave enones 4a,b , which were transformed into pyridines 6a,b , 8a,b , isoxazolines 9a,b , pyrazolines 10a–d , and pyrimidines 11a,b via several synthetic routes. Virtual screening was carried out by molecular modeling evaluation of the designed compounds. Biological evaluation of the prepared compounds showed that most of the synthesized compounds exhibit more than 50% growth inhibitory.

【 授权许可】

CC BY|CC BY-NC-ND