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Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity.
Liu, Yi-Chen; Yang, Ya-Dong; Liu, Wen-Qiang; Du, Ting-Ting; Wang, Ru; Ji, Ming; Yang, Bei-Bei; Li, Li; Chen, Xiao-Guang.
Afiliação
  • Liu YC; 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 Medica
  • Yang YD; 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 Medica
  • Liu WQ; 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 Medica
  • Du TT; 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 Medica
  • Wang R; 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 Medica
  • Ji M; 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 Medica
  • Yang BB; 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 Medica
  • Li L; 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 Medica
  • Chen XG; 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 Medica
Bioorg Med Chem ; 65: 116757, 2022 07 01.
Article em En | MEDLINE | ID: mdl-35504209
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias Hepáticas Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias Hepáticas Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article