Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
Identifieur interne : 001849 ( Main/Exploration ); précédent : 001848; suivant : 001850Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
Auteurs : Dmytro Havrylyuk [Ukraine] ; Borys Zimenkovsky ; Olexandr Vasylenko ; Craig W. Day ; Donald F. Smee ; Philippe Grellier ; Roman LesykSource :
- European journal of medicinal chemistry [ 1768-3254 ] ; 2013.
Descripteurs français
- KwdFr :
- Antinéoplasiques (), Antinéoplasiques (pharmacologie), Antinéoplasiques (synthèse chimique), Antiprotozoaires (), Antiprotozoaires (pharmacologie), Antiprotozoaires (synthèse chimique), Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Humains, Lignée cellulaire tumorale, Pyrazoles (), Relation structure-activité, Techniques de chimie synthétique, Thiazolidines (), Thiazolidines (pharmacologie), Thiazolidines (synthèse chimique), Trypanosoma brucei brucei (), Virus ().
- MESH :
- pharmacologie : Antinéoplasiques, Antiprotozoaires, Antiviraux, Thiazolidines.
- synthèse chimique : Antinéoplasiques, Antiprotozoaires, Antiviraux, Thiazolidines.
- Antinéoplasiques, Antiprotozoaires, Antiviraux, Humains, Lignée cellulaire tumorale, Pyrazoles, Relation structure-activité, Techniques de chimie synthétique, Thiazolidines, Trypanosoma brucei brucei, Virus.
English descriptors
- KwdEn :
- Antineoplastic Agents (chemical synthesis), Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Antiprotozoal Agents (chemical synthesis), Antiprotozoal Agents (chemistry), Antiprotozoal Agents (pharmacology), Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Cell Line, Tumor, Chemistry Techniques, Synthetic, Humans, Pyrazoles (chemistry), Structure-Activity Relationship, Thiazolidines (chemical synthesis), Thiazolidines (chemistry), Thiazolidines (pharmacology), Trypanosoma brucei brucei (drug effects), Viruses (drug effects).
- MESH :
- chemical , chemical synthesis : Antineoplastic Agents, Antiprotozoal Agents, Antiviral Agents, Thiazolidines.
- chemical , chemistry : Antineoplastic Agents, Antiprotozoal Agents, Antiviral Agents, Pyrazoles, Thiazolidines.
- chemical , pharmacology : Antineoplastic Agents, Antiprotozoal Agents, Antiviral Agents, Thiazolidines.
- drug effects : Trypanosoma brucei brucei, Viruses.
- Cell Line, Tumor, Chemistry Techniques, Synthetic, Humans, Structure-Activity Relationship.
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.
DOI: 10.1016/j.ejmech.2013.05.044
PubMed: 23811085
Affiliations:
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Le document en format XML
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Day</name></author><author><name sortKey="Smee, Donald F" sort="Smee, Donald F" uniqKey="Smee D" first="Donald F" last="Smee">Donald F. Smee</name></author><author><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name></author><author><name sortKey="Lesyk, Roman" sort="Lesyk, Roman" uniqKey="Lesyk R" first="Roman" last="Lesyk">Roman Lesyk</name></author></analytic><series><title level="j">European journal of medicinal chemistry</title><idno type="eISSN">1768-3254</idno><imprint><date when="2013" type="published">2013</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antineoplastic Agents (chemical synthesis)</term><term>Antineoplastic Agents (chemistry)</term><term>Antineoplastic Agents (pharmacology)</term><term>Antiprotozoal Agents (chemical synthesis)</term><term>Antiprotozoal Agents (chemistry)</term><term>Antiprotozoal Agents (pharmacology)</term><term>Antiviral Agents (chemical synthesis)</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacology)</term><term>Cell Line, Tumor</term><term>Chemistry Techniques, Synthetic</term><term>Humans</term><term>Pyrazoles (chemistry)</term><term>Structure-Activity Relationship</term><term>Thiazolidines (chemical synthesis)</term><term>Thiazolidines (chemistry)</term><term>Thiazolidines (pharmacology)</term><term>Trypanosoma brucei brucei (drug effects)</term><term>Viruses (drug effects)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques ()</term><term>Antinéoplasiques (pharmacologie)</term><term>Antinéoplasiques (synthèse chimique)</term><term>Antiprotozoaires ()</term><term>Antiprotozoaires (pharmacologie)</term><term>Antiprotozoaires (synthèse chimique)</term><term>Antiviraux ()</term><term>Antiviraux (pharmacologie)</term><term>Antiviraux (synthèse chimique)</term><term>Humains</term><term>Lignée cellulaire tumorale</term><term>Pyrazoles ()</term><term>Relation structure-activité</term><term>Techniques de chimie synthétique</term><term>Thiazolidines ()</term><term>Thiazolidines (pharmacologie)</term><term>Thiazolidines (synthèse chimique)</term><term>Trypanosoma brucei brucei ()</term><term>Virus ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antineoplastic Agents</term><term>Antiprotozoal Agents</term><term>Antiviral Agents</term><term>Thiazolidines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antineoplastic Agents</term><term>Antiprotozoal Agents</term><term>Antiviral Agents</term><term>Pyrazoles</term><term>Thiazolidines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antineoplastic Agents</term><term>Antiprotozoal Agents</term><term>Antiviral Agents</term><term>Thiazolidines</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Trypanosoma brucei brucei</term><term>Viruses</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antinéoplasiques</term><term>Antiprotozoaires</term><term>Antiviraux</term><term>Thiazolidines</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antinéoplasiques</term><term>Antiprotozoaires</term><term>Antiviraux</term><term>Thiazolidines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line, Tumor</term><term>Chemistry Techniques, Synthetic</term><term>Humans</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antinéoplasiques</term><term>Antiprotozoaires</term><term>Antiviraux</term><term>Humains</term><term>Lignée cellulaire tumorale</term><term>Pyrazoles</term><term>Relation structure-activité</term><term>Techniques de chimie synthétique</term><term>Thiazolidines</term><term>Trypanosoma brucei brucei</term><term>Virus</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">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.</div></front></TEI><affiliations><list><country><li>Ukraine</li></country></list><tree><noCountry><name sortKey="Day, Craig W" sort="Day, Craig W" uniqKey="Day C" first="Craig W" last="Day">Craig W. Day</name><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name><name sortKey="Lesyk, Roman" sort="Lesyk, Roman" uniqKey="Lesyk R" first="Roman" last="Lesyk">Roman Lesyk</name><name sortKey="Smee, Donald F" sort="Smee, Donald F" uniqKey="Smee D" first="Donald F" last="Smee">Donald F. Smee</name><name sortKey="Vasylenko, Olexandr" sort="Vasylenko, Olexandr" uniqKey="Vasylenko O" first="Olexandr" last="Vasylenko">Olexandr Vasylenko</name><name sortKey="Zimenkovsky, Borys" sort="Zimenkovsky, Borys" uniqKey="Zimenkovsky B" first="Borys" last="Zimenkovsky">Borys Zimenkovsky</name></noCountry><country name="Ukraine"><noRegion><name sortKey="Havrylyuk, Dmytro" sort="Havrylyuk, Dmytro" uniqKey="Havrylyuk D" first="Dmytro" last="Havrylyuk">Dmytro Havrylyuk</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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