Synthesis, cytotoxicities and DNA-binding affinities of benzofuran-3-ols and their fused analogs

Zhong Zhen Zhou, Min Zou, Jia Zhou, Chun Qiong Zhou, Yan Hong Deng, Ming Hui Chen, Chun Ping Gu, Zhi Hong JIANG, Wen Hua Chen*, Shu Wen Liu

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

12 Citations (Scopus)


A series of benzofuropyrazoles 2a-i were synthesized in 10-92% from the reaction of 2-aroylbenzofuran-3-ols 1a-i with hydrazine hydrate, and screened for their antitumor activities toward four human solid tumor cell lines, including gastric carcinoma cells MKN45, hepatocellular carcinoma cells HepG2, breast cancer cells MCF-7, and lung cancer cells A549. The results indicated that both compounds 1a-i and 2a-i displayed moderate antitumor activities. Among them, compound 2e exhibited potent inhibitory activity toward all the four tumor cell lines. In addition, compounds 1e and 2e showed strong DNA-binding affinities, and induced an increase in the viscosity of calf-thymus DNA, suggesting that they might act as an intercalator.

Original languageEnglish
Pages (from-to)1057-1061
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Issue number8
Publication statusPublished - Aug 2011

Scopus Subject Areas

  • Chemistry(all)
  • Drug Discovery

User-Defined Keywords

  • Benzofuran
  • Benzofuropyrazole
  • Cytotoxicity
  • DNA binding


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