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Synthesis and biological evaluation of farnesylthiosalicylamides as potential anti-tumor agents
- Source :
- Bioorganicmedicinal chemistry. 22(1)
- Publication Year :
- 2013
-
Abstract
- Fourteen hybrids of farnesylthiosalicylic acid (FTS) with various diamines were synthesized and biologically evaluated. It was found that FTS-monoamide molecules (10a-g) displayed strong anti-proliferative activity against seven human cancer cell lines, superior to FTS and FTS-bisamide compounds (11a-g). The mono-amide 10f was the most active, with IC₅₀s of 3.78-7.63 μM against all tested cancer cells, even more potent than sorafenib (9.12-22.9 μM). In addition, 10f induced SMMC-7721 cell apoptosis, down-regulated the expression of Bcl-2 and up-regulated Bax and caspase-3. Furthermore, 10f had the improved aqueous solubility relative to FTS. Finally, treatment with 10f dose-dependently inhibited the Ras-related signaling pathways in SMMC-7721 cells. Collectively, 10f could be a promising candidate for the intervention of human cancers.
- Subjects :
- Sorafenib
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
Biochemistry
Neoplasms
Drug Discovery
medicine
Humans
Molecular Biology
Biological evaluation
Antitumor activity
Chemistry
Organic Chemistry
Farnesylthiosalicylic acid
Farnesol
Salicylates
Cell culture
Cancer cell
Cancer research
Molecular Medicine
Signal transduction
medicine.drug
Signal Transduction
Subjects
Details
- ISSN :
- 14643391
- Volume :
- 22
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry
- Accession number :
- edsair.doi.dedup.....dc75962ec2f5ab364339792950adcfce