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

Bioorganic & Medicinal Chemistry
2022.0

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.

DOI： 10.1016/j.bmc.2022.116757

Knowledge Graph

Similar Paper

Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity
Bioorganic & Medicinal Chemistry 2022.0
Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors
European Journal of Medicinal Chemistry 2021.0
N -Arylsulfonylsubstituted- 1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin
Bioorganic & Medicinal Chemistry 2018.0
Structure–Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors
ACS Medicinal Chemistry Letters 2021.0
N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling
Journal of Medicinal Chemistry 2015.0
Antagonizing STAT3 activation with benzo[b]thiophene 1, 1-dioxide based small molecules
European Journal of Medicinal Chemistry 2017.0
Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation
European Journal of Medicinal Chemistry 2016.0
Novel synthetic bisindolylmaleimide alkaloids inhibit STAT3 activation by binding to the SH2 domain and suppress breast xenograft tumor growth
Oncogene 2018.0
In pursuit of a selective hepatocellular carcinoma therapeutic agent: Novel thalidomide derivatives with antiproliferative, antimigratory and STAT3 inhibitory properties
European Journal of Medicinal Chemistry 2021.0
Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents
MedChemComm 2017.0