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A Novel Method to Synthesize 4-Aryl-1H-1,2,3-Triazoles and its Antihepatoma Activity.
- Source :
-
Anti-cancer agents in medicinal chemistry [Anticancer Agents Med Chem] 2016; Vol. 16 (12), pp. 1622-1627. - Publication Year :
- 2016
-
Abstract
- A novel synthetic method of 4-substituted aryl-1H-1,2,3-triazoles from arylglyoxaldoxime semicarbazone with sodium dithionite and O2 was found to be safer than the Huisgen azide- alkyne dipolar cycloaddition. A total of 17 new structures of 4-substituted aryl-1H-1,2,3- triazoles were characterized by 1H NMR, 13C NMR, ESI-MS. Subsequently, their in vitro antihepatoma activities were evaluated on human hepatoma QGY-7703, Bel-7402 and SMMC-7721 cell lines and mouse fibroblast cells L-929 by MTS assay. Among them, 5k exhibited excellent activity against QGY-7703 (GI50 = 0.0232 μM), while 5p and 5q displayed good activity (GI50 = 0.103 μM and GI50 = 0.182 μM) against the growth of SMMC-7721 cell lines. Furthermore, 5k, 5p and 5q showed slight selectivity of inhibition on hepatoma cell lines over normal cell line L-929.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Carcinoma, Hepatocellular pathology
Cell Line, Tumor
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Liver Neoplasms pathology
Molecular Structure
Structure-Activity Relationship
Triazoles chemical synthesis
Triazoles chemistry
Antineoplastic Agents pharmacology
Carcinoma, Hepatocellular drug therapy
Liver Neoplasms drug therapy
Triazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1875-5992
- Volume :
- 16
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Anti-cancer agents in medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26592747
- Full Text :
- https://doi.org/10.2174/1871520616666151123095646