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Synthesis and biological evaluation of 3-hydroxymethyl-5-(1H-1,2,3-triazol) isoxazolidines
- Publication Year :
- 2013
-
Abstract
- A synthetic approach towards a series of 3-hydroxymethyl-5-(1 H- 1,2,3-triazol)isoxazolidines has been reported, according to a procedure based on the cycloaddition reaction, under microwave irradiation, of a nitrone with 1-vinyl triazoles, prepared by a click reaction of azides with alkynes. Biological tests show that the synthesized compounds are able to inhibit proliferation of follicular and anaplastic human thyroid cancer cell lines, with IC 50 values ranging from 3.87 to 8.76 μM. The obtained compounds induce caspase-3 activation and DNA fragmentation prevalently in follicular human thyroid cancer cell lines.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
modified nucleosides
DNA Fragmentation
Biochemistry
antitumor agents
Nitrone
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
Tumor Cells, Cultured
Humans
Hydroxymethyl
FTC-133 and 8305C cell lines
Molecular Biology
Cell Proliferation
Biological evaluation
chemistry.chemical_classification
Dose-Response Relationship, Drug
Molecular Structure
Caspase 3
Chemistry
Organic Chemistry
Isoxazoles
Triazoles
Combinatorial chemistry
Modified nucleosides
Click-chemistry
Antitumor agents
1.3-Dipolar cycloaddition
Cycloaddition
1,3-Dipolar cycloaddition
Click chemistry
Molecular Medicine
DNA fragmentation
Human thyroid
Drug Screening Assays, Antitumor
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....62c7006e1b9c7294391675b1a9a98603