TY - JOUR
T1 - Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
AU - Havrylyuk, Dmytro
AU - Zimenkovsky, Borys
AU - Vasylenko, Olexandr
AU - Day, Craig W.
AU - Smee, Donald F.
AU - Grellier, Philippe
AU - Lesyk, Roman
N1 - Publisher Copyright:
© 2013 Elsevier Masson SAS.
PY - 2013/8
Y1 - 2013/8
N2 - 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.
AB - 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.
KW - 4-Thiazolidinones
KW - Anticancer activity
KW - Antitrypanosomal activity
KW - Antiviral activity
KW - Pyrazolines
KW - Synthesis
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U2 - 10.1016/j.ejmech.2013.05.044
DO - 10.1016/j.ejmech.2013.05.044
M3 - Article
C2 - 23811085
AN - SCOPUS:84879470955
SN - 0223-5234
VL - 66
SP - 228
EP - 237
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -