Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones

Dmytro Havrylyuk, Borys Zimenkovsky, Olexandr Vasylenko, Craig W. Day, Donald F. Smee, Philippe Grellier, Roman Lesyk

Research output: Contribution to journalArticlepeer-review

78 Scopus citations


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 languageEnglish
Pages (from-to)228-237
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
StatePublished - Aug 2013

Bibliographical note

Funding Information:
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.

Publisher Copyright:
© 2013 Elsevier Masson SAS.


  • 4-Thiazolidinones
  • Anticancer activity
  • Antitrypanosomal activity
  • Antiviral activity
  • Pyrazolines
  • Synthesis

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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