Synthesis and biological activity of fused furo[2,3-d]pyrimidinone derivatives as analgesic and antitumor agents

Qing Li, Yong Mei Chen, Yang Gen Hu*, Xin Luo, Joshua KO, Chi Wai Cheung

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

Tumor growth is usually associated with persistent pain, especially during mid and terminal stages of cancer development. Nonetheless, a medicinal compound that possesses both anticancer and analgesic properties has not been identified. The 2-alkylthio-benzofuro[3,2-d]pyrimidin-4(3H)-ones (Code 5a-d) and 1-aryl-2-alkylthio-benzofuro[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-ones (Code 10a-g) were synthesized by using the bioisostere concept, which were obtained via the aza-Wittig reaction of functionalized iminophosphoranes reacted with carbon disulfide and further reaction of the product with alkyl halides or halogenated aliphatic esters. The analgesic properties of 5a-d and 10a-g were studied using rat chronic constriction injury model and the antitumor properties of these chemicals were assessed using MTS cell proliferation assay. Results showed that 5a-d and 10a-g were found to attenuate thermal and mechanical allodynia induced by neuropathy and inhibited the proliferation of three human cancer cell lines (A459, HepG2, and HeLa). Among these compounds, 10g showed highly positive effects in both assessments, and would be selected for future work.

Original languageEnglish
Pages (from-to)939-949
Number of pages11
JournalResearch on Chemical Intermediates
Volume42
Issue number2
DOIs
Publication statusPublished - 1 Feb 2016

Scopus Subject Areas

  • Chemistry(all)

User-Defined Keywords

  • Analgesic and antitumor
  • Fused furo[2,3-d]pyrimidinone derivatives
  • Synthesis

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