Synthesis and anticancer and antiviral activities of new 2-pyrazoline-substituted 4-thiazolidinones

Dmytro Havrylyuk, Borys Zimenkovsky, Olexandr Vasylenko, Roman Lesyk

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39 Scopus citations

Abstract

2-(4,5-Dihydropyrazol-1-yl)-thiazol-4-ones (2-5) have been synthesized starting from 3-phenyl-5-aryl-1-thiocarbamoyl-2-pyrazolines via [2+3]-cyclization with 2-bromopropionic acid, maleic anhydride, N-arylmaleimides, and aroylacrylic acids. The in vitro anticancer activity of, and were tested by the National Cancer Institute. Compounds, and demonstrated selective inhibition of leukemia cell lines growth at a single concentration (10-5 M). The screening of antiviral activity for a broad panel of viruses revealed that N-(4-methoxyphenyl)-2-{2-[5-(4-methoxyphenyl)-3-phenyl-4, 5-dihydropyrazol-1-yl]-4-oxo-4,5-dihydrothiazol-5-yl}-acetamide was highly active against Tacaribe TRVL 11 573 virus strain (EC50 = 0.71 μg/mL, selectivity index = 130).

Original languageEnglish
Pages (from-to)E55-E62
JournalJournal of Heterocyclic Chemistry
Volume50
Issue numberSUPPL.1
DOIs
StatePublished - Feb 2013

ASJC Scopus subject areas

  • Organic Chemistry

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