Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
Identifieur interne : 002699 ( Ncbi/Merge ); précédent : 002698; suivant : 002700Synthesis 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
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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><pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">23811085</PMID><DateCompleted><Year>2014</Year><Month>02</Month><Day>28</Day></DateCompleted><DateRevised><Year>2020</Year><Month>04</Month><Day>07</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1768-3254</ISSN><JournalIssue CitedMedium="Internet"><Volume>66</Volume><PubDate><Year>2013</Year><Month>Aug</Month></PubDate></JournalIssue><Title>European journal of medicinal chemistry</Title><ISOAbbreviation>Eur J Med Chem</ISOAbbreviation></Journal><ArticleTitle>Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.</ArticleTitle><Pagination><MedlinePgn>228-37</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1016/j.ejmech.2013.05.044</ELocationID><ELocationID EIdType="pii" ValidYN="Y">S0223-5234(13)00362-0</ELocationID><Abstract><AbstractText>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.</AbstractText><CopyrightInformation>Copyright © 2013 Elsevier Masson SAS. All rights reserved.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Havrylyuk</LastName><ForeName>Dmytro</ForeName><Initials>D</Initials><AffiliationInfo><Affiliation>Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, Lviv 79010, Ukraine.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Zimenkovsky</LastName><ForeName>Borys</ForeName><Initials>B</Initials></Author><Author ValidYN="Y"><LastName>Vasylenko</LastName><ForeName>Olexandr</ForeName><Initials>O</Initials></Author><Author ValidYN="Y"><LastName>Day</LastName><ForeName>Craig W</ForeName><Initials>CW</Initials></Author><Author ValidYN="Y"><LastName>Smee</LastName><ForeName>Donald F</ForeName><Initials>DF</Initials></Author><Author ValidYN="Y"><LastName>Grellier</LastName><ForeName>Philippe</ForeName><Initials>P</Initials></Author><Author ValidYN="Y"><LastName>Lesyk</LastName><ForeName>Roman</ForeName><Initials>R</Initials></Author></AuthorList><Language>eng</Language><GrantList CompleteYN="Y"><Grant><GrantID>N01AI15435</GrantID><Acronym>AI</Acronym><Agency>NIAID NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>N01-AI-15435</GrantID><Acronym>AI</Acronym><Agency>NIAID NIH HHS</Agency><Country>United States</Country></Grant></GrantList><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType><PublicationType UI="D052061">Research Support, N.I.H., Extramural</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2013</Year><Month>06</Month><Day>06</Day></ArticleDate></Article><MedlineJournalInfo><Country>France</Country><MedlineTA>Eur J Med Chem</MedlineTA><NlmUniqueID>0420510</NlmUniqueID><ISSNLinking>0223-5234</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000970">Antineoplastic Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000981">Antiprotozoal Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000998">Antiviral Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D011720">Pyrazoles</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D053778">Thiazolidines</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName UI="D000970" MajorTopicYN="N">Antineoplastic Agents</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="N">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D000981" MajorTopicYN="N">Antiprotozoal 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MajorTopicYN="N">Pyrazoles</DescriptorName><QualifierName UI="Q000737" MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D013329" MajorTopicYN="N">Structure-Activity Relationship</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D053778" MajorTopicYN="N">Thiazolidines</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="Y">chemical synthesis</QualifierName><QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D014346" MajorTopicYN="N">Trypanosoma brucei brucei</DescriptorName><QualifierName UI="Q000187" MajorTopicYN="N">drug effects</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D014780" MajorTopicYN="N">Viruses</DescriptorName><QualifierName UI="Q000187" MajorTopicYN="N">drug effects</QualifierName></MeshHeading></MeshHeadingList><KeywordList Owner="NOTNLM"><Keyword 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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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