A green approach toward quinoxalines and bis-quinoxalines and their biological evaluation against A431, human skin cancer cell lines

作者：Bandyopadhyay Debasish; Cruz Jessica; Morales Liza D; Arman Hadi D; Cuate Erica; Lee Young S; Banik Bimal K^*; Kim Dae J

来源：Future Medicinal Chemistry, 2013, 5(12): 1377-1390.

DOI：10.4155/fmc.13.101

Background: The objective of this study was to develop a practical green procedure to synthesize quinoxalines and bis-quinoxalines and evaluate their inhibitory effects on the viability of A431 human epidermoid carcinoma cells. Method: A series of quinoxaline and bis-quinoxaline derivatives have been designed and synthesized following a microwave-assisted and bismuth nitrate-catalyzed eco-friendly route. A detailed comparison has been made between microwave-induced protocol with the reactions occurred at room temperature. The structure of the compounds have been elucidated by various spectroscopic methods and finally confirmed by x-ray crystallographic analyses. Results: Two quinoxaline derivatives, compounds 6 and 12 have demonstrated inhibitory effects on the viability of A431 human epidermoid carcinoma cells when compared with HaCaT nontumorigenic human keratinocyte cells. Conclusion: Notably, compound 6 inhibits Stat3 phosphorylation/activation in A431 skin cancer cells.

• 出版日期2013-8