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Novel dibenzo[b,d]furan-1H-1,2,4-triazole derivatives: Synthesis and antitumor activity
- Source :
- Scopus-Elsevier
- Publication Year :
- 2015
-
Abstract
- Twenty-four new dibenzo[b,d]furan-1H-1,2,4-triazole derivatives were synthesized and investigated for in vitro cytotoxic activity against five tumor cell lines. The results show that the substitution at 4-position of the 1,2,4-triazole with a benzyl, 4-bromophenacyl or naphthylacyl group could be crucial for prommoting cytotoxic activity. Especially, compound 28 was found to be the most powerful derivative with IC50 values lower than 3.50 μM against five investigated tumor cell lines, while compound 19 showed selective activity against leukemia (HL-60) and breast carcinoma (MCF-7) cell lines with IC50 values of 0.80 and 1.76 μM, respectively. Compound 19 can induce cell cycle arrest at G2/M phase and apoptosis in SMMC-7721 cells.
- Subjects :
- Cancer Research
Cell cycle checkpoint
Stereochemistry
Antineoplastic Agents
Apoptosis
HL-60 Cells
Bioinformatics
01 natural sciences
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
Furan
Benzyl Compounds
Structure–activity relationship
Cytotoxic T cell
Humans
Furans
Cell Proliferation
Pharmacology
010405 organic chemistry
1,2,4-Triazole
Triazoles
In vitro
0104 chemical sciences
G2 Phase Cell Cycle Checkpoints
010404 medicinal & biomolecular chemistry
chemistry
Cell culture
MCF-7 Cells
Molecular Medicine
Subjects
Details
- ISSN :
- 18755992
- Volume :
- 16
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Anti-cancer agents in medicinal chemistry
- Accession number :
- edsair.doi.dedup.....f787784db09225381a86c3ac1bd56ef8