期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 66, 期 -, 页码 228-237出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.05.044
关键词
Synthesis; Pyrazolines; 4-Thiazolidinones; Anticancer activity; Antitrypanosomal activity; Antiviral activity
资金
- Virology Branch, Division of Microbiology and Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD, USA [N01-AI-15435]
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [N01AI015435] Funding Source: NIH RePORTER
A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensitivity profile toward the leukemia subpanel cell lines with GI(50) value ranges of 2.12-4.58 mu M (4d) and 1.64-3.20 mu M (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Tiypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses. (C) 2013 Elsevier Masson SAS. All rights reserved.
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