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New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-kappa B transcription factors
- Source :
- Journal of Enzyme Inhibition and Medicinal Chemistry, Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 1012-1028 (2017)
- Publication Year :
- 2017
- Publisher :
- Taylor and Francis Ltd, 2017.
-
Abstract
- A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most of the new hybrid compounds were able to strongly and selectively bind to STAT3, whereas the parent drugs were devoid of this ability at the tested concentrations. Some of them were also able to inhibit the NF-κB transcriptional activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro with IC50 in micromolar range, thus suggesting a potential anticancer activity. Taken together, our study described the identification of new derivatives with dual STAT3/NF-κB inhibitory activity, which may represent hit compounds for developing multi-target anticancer agents.
- Subjects :
- NF-κB inhibitors
STAT3 Transcription Factor
Pharmacology
STAT3 inhibitors
Dose-Response Relationship, Drug
NF-κB inhibitors
Cell Survival
Drug Discovery3003 Pharmaceutical Science
lcsh:RM1-950
NF-kappa B
Anticancer drug
Sulfuric Acids
HCT116 Cells
cytotoxicity
methanethiosulfonate derivatives
Cinnamates
Diterpenes
HeLa Cells
Humans
Structure-Activity Relationship
Dose-Response Relationship
lcsh:Therapeutics. Pharmacology
Drug
Research Paper
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Journal of Enzyme Inhibition and Medicinal Chemistry, Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 1012-1028 (2017)
- Accession number :
- edsair.pmid.dedup....9f308cd94b582b5b3c69d64aa02f3b9c