Abstract
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 GI50 value ranges of 2.12-4.58 μM (4d) and 1.64-3.20 μM (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2-yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Trypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses.
| Original language | English |
|---|---|
| Pages (from-to) | 228-237 |
| Number of pages | 10 |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 66 |
| DOIs | |
| State | Published - Aug 2013 |
Bibliographical note
Publisher Copyright:© 2013 Elsevier Masson SAS.
Funding
We are grateful to Dr. V.L. Narayanan from Drug Synthesis and Chemistry Branch, National Cancer Institute, Bethesda, MD, USA, for in vitro evaluation of anticancer activity. Evaluations of compounds for antiviral activity were supported by funds from contract N01-AI-15435 from the Virology Branch, Division of Microbiology and Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, MD, USA.
| Funders | Funder number |
|---|---|
| National Institutes of Health (NIH) | |
| National Institute of Allergy and Infectious Diseases | N01AI015435 |
| European Society of Clinical Microbiology and Infectious Diseases |
Keywords
- 4-Thiazolidinones
- Anticancer activity
- Antitrypanosomal activity
- Antiviral activity
- Pyrazolines
- Synthesis
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
- Organic Chemistry