2. Academic Validation
  3. Design, synthesis and structure-activity relationship of novel quinoxaline derivatives as cancer chemopreventive agent by inhibition of tyrosine kinase receptor

Design, synthesis and structure-activity relationship of novel quinoxaline derivatives as cancer chemopreventive agent by inhibition of tyrosine kinase receptor

  • Eur J Med Chem. 2013 Nov:69:115-24. doi: 10.1016/j.ejmech.2013.07.049.
Shadia A Galal 1,  Ahmed S Abdelsamie,  Salwa M Soliman,  Jeremie Mortier,  Gerhard Wolber,  Mamdouh M Ali,  Harukuni Tokuda,  Nobutaka Suzuki,  Akira Lida,  Raghda A Ramadan,  Hoda I El Diwani
Affiliations

Affiliation

  • 1 Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries, National Research Center, Dokki, 12622 Cairo, Egypt. Electronic address: sh12galal@yahoo.com.
PMID: 24013411 DOI: 10.1016/j.ejmech.2013.07.049
Abstract

The Cancer chemopreventive activity of quinoxaline derivatives 1-20 has been evaluated by studying the inhibitory effect on Epstein-Barr virus early antigen (EBV-EA) activation. The quinoxaline derivatives 1-20 showed inhibitory effect on EBV-EA activation without cytotoxicity on Raji cells. All compounds exhibited dose dependent inhibitory activities, most of them showed significant activity at 1000 mol ratio/12-O-tetradecanoylphorbol-13-acetate (TPA). Compounds 7 and 9 exhibited stronger inhibitory effects on the EBV-EA activation than that of the representative control, oleanolic acid, at the highest measured concentration. In addition, compounds 7-10 showed potent and selective inhibition of human tyrosine kinase (Trk) in liver Cancer HepG2 and breast Cancer MCF-7 cell lines similar to the positive control, doxorubicin.

Keywords

Cancer chemopreventive activity; Docking; Epstein–Barr virus; Protein tyrosine kinase; Quinoxalines; Synthesis.

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