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

• DOI: 10.1016/j.ejmech.2013.05.044
• Publication Date: 2013-06-06T17:15:58Z
• Authors: Dmytro Havrylyuk; Borys Zimenkovsky; Olexandr Vasylenko; Craig W. Day; Donald F. Smee; Philippe Grellier; Roman Lesyk
• Keywords: 0303 health sciences; [SDV]Life Sciences [q-bio]; Trypanosoma brucei brucei; Antiprotozoal Agents; Antineoplastic Agents; Chemistry Techniques, Synthetic; Antiviral Agents; 3. Good health; [SDV] Life Sciences [q-bio]; Structure-Activity Relationship; 03 medical and health sciences; [SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology; Cell Line, Tumor; [CHIM] Chemical Sciences; Viruses; [CHIM]Chemical Sciences; Humans; Pyrazoles; Thiazolidines; Original Article; [SDV.MP] Life Sciences [q-bio]/Microbiology and Parasitology

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.