2. Academic Validation
  3. Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity

Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity

  • Bioorg Med Chem. 2022 Jul 1;65:116757. doi: 10.1016/j.bmc.2022.116757.
Yi-Chen Liu 1,  Ya-Dong Yang 1,  Wen-Qiang Liu 1,  Ting-Ting Du 1,  Ru Wang 1,  Ming Ji 1,  Bei-Bei Yang 1,  Li Li 2,  Xiao-Guang Chen 3
Affiliations

Affiliations

  • 1 Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
  • 2 Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. Electronic address: annaleelin@imm.ac.cn.
  • 3 Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. Electronic address: chxg@imm.ac.cn.
PMID: 35504209 DOI: 10.1016/j.bmc.2022.116757
Abstract

Polycyclic aromatic systems have been considered good biological probes, but some may also be good scaffolds for drug development. In this study, a series of benzobis(imidazole) derivatives were identified as STAT3 signal inhibitors, among which compound 24 showed significant inhibition of IL-6 induced JAK/STAT3 signalling pathway activation. Moreover, 24 inhibited Cancer cell growth and migration, and induced cell Apoptosis as well as cycle arrest in human hepatocellular carcinoma cells (HepG2) and oesophageal carcinoma cells (EC109). Compound 24 also displayed obvious antitumor activity in a mouse HepG2 cell xenograft tumor model without affecting the body weight. These results confirmed that 24 was a potential STAT3 signal inhibitor with certain antitumor activity.

Keywords

Antitumor; Benzobis(imidazole); IL-6/JAK/STAT3 signalling pathway; STAT3.

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