ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Synthesis and characterization of furazan derivatives and their evaluation as antitumor agents

Taiping Chen, Jianjun Zhou, Zicheng Li, Wencai Huang, Youfu Luo, and Yinglan Zhao

Sichuan University, Chengdu, People’s Republic of China

E-mail: sculzc@scu.edu.cn

Abstract: In order to discover compounds with better biological activity, a series of furazan derivatives were synthesized based on the structural modification of INCB024360 (Epacadostat). The anti-proliferative activities of new synthesized compounds 4a–o were screened in vitro against a panel of four human solid tumor cell lines (HepG2; A549, Hela and A375). We also reported the toxicity of compounds with low IC₅₀ values on human hepatic cell line (LO2), and the apoptosis effect of compounds 4h and 4i on Hela cell. The results showed that several compounds displayed good inhibitory activity, even better than the positive compound 5-fluorouracil (5-FU) for specific cell lines. In addition, the toxicity of compounds 4h–j and 4m–o towards LO2 were lower than the positive compound 5-FU.

Keywords: Furazan derivative ; Anti-proliferative activity ; Boulton–Katritzky rearrangement 

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-019-00834-6

Chemical Papers 73 (11) 2813–2820 (2019)