Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway

Ying Rui Yang, Jin Lian Wei, Xiao Fei Mo, Zhen Wei Yuan, Jia Lin Wang, Chao Zhang, Yi Yue Xie, Qi Dong You, Hao Peng Sun

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14 Citations (Scopus)


p53-independent malignant cancer is still severe health problem of human beings. HIF-1 pathway is believed to play an important role in the survival and developing progress of such cancers. In the present study, with the aim to inhibit the proliferation of p53-independent malignant cells, we disclose the optimization of 6a, the starting compound which is discovered in the screening of in-house compound collection. The structure-activity relationship (SAR) is summarized. The most potent derivative 8d, inhibits the proliferation of both p53-null and p53-mutated cells through inhibition of HIF-1 pathway. Our findings here provide a new chemotype in designing potent anticancer agent especially against those p53-independent malignant tumors.

Original languageEnglish
Pages (from-to)2713-2718
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number11
Publication statusPublished - 1 Jun 2016
Externally publishedYes


  • Antitumor
  • Apoptosis
  • Benzofuran
  • Cycle arrest
  • HIF-1 inhibition

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