Exploration of (hetero)aryl Derived Thienylchalcones for Antiviral and Anticancer Activities.
Identifieur interne : 001E41 ( Ncbi/Merge ); précédent : 001E40; suivant : 001E42Exploration of (hetero)aryl Derived Thienylchalcones for Antiviral and Anticancer Activities.
Auteurs : Vikrant Patil [Inde] ; Siddappa A. Patil [Inde] ; Renukadevi Patil [États-Unis] ; Alejandro Bugarin [États-Unis] ; Kenneth Beaman [États-Unis] ; Shivaputra A. Patil [États-Unis]Source :
- Medicinal chemistry (Shariqah (United Arab Emirates)) [ 1875-6638 ] ; 2019.
Descripteurs français
- KwdFr :
- MESH :
English descriptors
- KwdEn :
- MESH :
- chemical , chemistry : Antineoplastic Agents, Antiviral Agents, Chalcones.
- chemical , pharmacology : Antineoplastic Agents, Antiviral Agents, Chalcones.
- drug effects : Viruses.
- Cell Line, Tumor, Drug Evaluation, Preclinical, Humans.
Abstract
Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents.
DOI: 10.2174/1573406414666180524074648
PubMed: 29792154
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Patil</name><affiliation wicri:level="1"><nlm:affiliation>Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.</nlm:affiliation><country xml:lang="fr">Inde</country><wicri:regionArea>Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112</wicri:regionArea><wicri:noRegion>Bangalore 562112</wicri:noRegion></affiliation></author><author><name sortKey="Patil, Renukadevi" sort="Patil, Renukadevi" uniqKey="Patil R" first="Renukadevi" last="Patil">Renukadevi Patil</name><affiliation wicri:level="2"><nlm:affiliation>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064</wicri:regionArea><placeName><region type="state">Illinois</region></placeName></affiliation></author><author><name sortKey="Bugarin, Alejandro" sort="Bugarin, Alejandro" uniqKey="Bugarin A" first="Alejandro" last="Bugarin">Alejandro Bugarin</name><affiliation wicri:level="2"><nlm:affiliation>Department of Chemistry & Biochemistry, University of Texas at Arlington, Arlington, TX 76019, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Chemistry & Biochemistry, University of Texas at Arlington, Arlington, TX 76019</wicri:regionArea><placeName><region type="state">Texas</region></placeName></affiliation></author><author><name sortKey="Beaman, Kenneth" sort="Beaman, Kenneth" uniqKey="Beaman K" first="Kenneth" last="Beaman">Kenneth Beaman</name><affiliation wicri:level="2"><nlm:affiliation>Department of Microbiology and Immunology, Chicago Medical School, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Microbiology and Immunology, Chicago Medical School, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064</wicri:regionArea><placeName><region type="state">Illinois</region></placeName></affiliation></author><author><name sortKey="Patil, Shivaputra A" sort="Patil, Shivaputra A" uniqKey="Patil S" first="Shivaputra A" last="Patil">Shivaputra A. Patil</name><affiliation wicri:level="2"><nlm:affiliation>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064</wicri:regionArea><placeName><region type="state">Illinois</region></placeName></affiliation></author></analytic><series><title level="j">Medicinal chemistry (Shariqah (United Arab Emirates))</title><idno type="eISSN">1875-6638</idno><imprint><date when="2019" type="published">2019</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antineoplastic Agents (chemistry)</term><term>Antineoplastic Agents (pharmacology)</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacology)</term><term>Cell Line, Tumor</term><term>Chalcones (chemistry)</term><term>Chalcones (pharmacology)</term><term>Drug Evaluation, Preclinical</term><term>Humans</term><term>Viruses (drug effects)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques ()</term><term>Antinéoplasiques (pharmacologie)</term><term>Antiviraux ()</term><term>Antiviraux (pharmacologie)</term><term>Chalcones ()</term><term>Chalcones (pharmacologie)</term><term>Humains</term><term>Lignée cellulaire tumorale</term><term>Virus ()</term><term>Évaluation préclinique de médicament</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antineoplastic Agents</term><term>Antiviral Agents</term><term>Chalcones</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antineoplastic Agents</term><term>Antiviral Agents</term><term>Chalcones</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Viruses</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antinéoplasiques</term><term>Antiviraux</term><term>Chalcones</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line, Tumor</term><term>Drug Evaluation, Preclinical</term><term>Humans</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antinéoplasiques</term><term>Antiviraux</term><term>Chalcones</term><term>Humains</term><term>Lignée cellulaire tumorale</term><term>Virus</term><term>Évaluation préclinique de médicament</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents.</div></front></TEI><pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">29792154</PMID><DateCompleted><Year>2019</Year><Month>03</Month><Day>04</Day></DateCompleted><DateRevised><Year>2019</Year><Month>03</Month><Day>04</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1875-6638</ISSN><JournalIssue CitedMedium="Internet"><Volume>15</Volume><Issue>2</Issue><PubDate><Year>2019</Year></PubDate></JournalIssue><Title>Medicinal chemistry (Shariqah (United Arab Emirates))</Title><ISOAbbreviation>Med Chem</ISOAbbreviation></Journal><ArticleTitle>Exploration of (hetero)aryl Derived Thienylchalcones for Antiviral and Anticancer Activities.</ArticleTitle><Pagination><MedlinePgn>150-161</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.2174/1573406414666180524074648</ELocationID><Abstract><AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents.</AbstractText><AbstractText Label="OBJECTIVE" NlmCategory="OBJECTIVE">With the aim of identifying the broad acting antiviral and anticancer agents, we discovered substituted aryl/heteroaryl derived thienyl chalcones as antiviral and anticancer agents.</AbstractText><AbstractText Label="METHOD" NlmCategory="METHODS">A focused set of thienyl chalcone derivaties II-VI was screened for selected viruses Hepatitis B virus (HBV), Herpes simplex virus 1 (HSV-1), Human cytomegalovirus (HCMV), Dengue virus 2 (DENV2), Influenza A (H1N1) virus, MERS coronavirus, Poliovirus 1 (PV 1), Rift Valley fever (RVF), Tacaribe virus (TCRV), Venezuelan equine encephalitis virus (VEE) and Zika virus (ZIKV) using the National Institute of Allergy and Infectious Diseases (NIAID)'s Division of Microbiology and Infectious Diseases (DMID) antiviral screening program. Additionally, a cyclopropylquinoline derivative IV has been screened for 60 human cancer cell lines using the Development Therapeutics Program (DTP) of NCI.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">All thienyl chalcone derivatives II-VI displayed moderate to excellent antiviral activity towards several viruses tested. Compounds V and VI were turned out be active compounds towards human cytomegalovirus for both normal strain (AD169) as well as resistant isolate (GDGr K17). Particularly, cyano derivative V showed very high potency (EC50: <0.05 µM) towards AD169 strain of HCMV compared to standard drug Ganciclovir (EC50: 0.12 µM). Additionally, it showed moderate activity in the secondary assay (AD169; EC50: 2.30 µM). The cyclopropylquinoline derivative IV displayed high potency towards Rift Valley fever virus (RVFV) and Tacaribe virus (TCRV) towards Rift Valley fever virus (RVFV). The cyclopropylquinoline derivative IV is nearly 28 times more potent in our initial in vitro visual assay (EC50: 0.39 µg/ml) and nearly 17 times more potent in neutral red assay (EC50: 0.71 μg/ml) compared to the standard drug Ribavirin (EC50: 11 µg/ml; visual assay and EC50: 12 µg/ml; neutral red assay). It is nearly 12 times more potent in our initial in vitro visual assay (EC50: >1 µg/ml) and nearly 8 times more potent in neutral red assay (EC50: >1.3 µg/ml) compared to the standard drug Ribavirin (EC50: 12 µg/ml; visual assay and EC50: 9.9 µg/ml; neutral red assay) towards Tacaribe virus (TCRV). Additionally, cyclopropylquinoline derivative IV has shown strong growth inhibitory activity towards three major cancers (colon, breast, and leukemia) cell lines and moderate growth inhibition shown towards other cancer cell lines screened.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Compounds V and VI were demonstrated viral inhibition towards Human cytomegalovirus, whereas cyclopropylquinoline derivative IV towards Rift Valley fever virus and Tacaribe virus. Additionally, cyclopropylquinoline derivative IV has displayed very good cytotoxicity against colon, breast and leukemia cell lines in vitro.</AbstractText><CopyrightInformation>Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Patil</LastName><ForeName>Vikrant</ForeName><Initials>V</Initials><AffiliationInfo><Affiliation>Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Patil</LastName><ForeName>Siddappa A</ForeName><Initials>SA</Initials><AffiliationInfo><Affiliation>Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Patil</LastName><ForeName>Renukadevi</ForeName><Initials>R</Initials><AffiliationInfo><Affiliation>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Bugarin</LastName><ForeName>Alejandro</ForeName><Initials>A</Initials><AffiliationInfo><Affiliation>Department of Chemistry & Biochemistry, University of Texas at Arlington, Arlington, TX 76019, United States.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Beaman</LastName><ForeName>Kenneth</ForeName><Initials>K</Initials><AffiliationInfo><Affiliation>Department of Microbiology and Immunology, Chicago Medical School, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Patil</LastName><ForeName>Shivaputra A</ForeName><Initials>SA</Initials><AffiliationInfo><Affiliation>Pharmaceutical Sciences Department, College of Pharmacy, Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL 60064, United States.</Affiliation></AffiliationInfo></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>Netherlands</Country><MedlineTA>Med Chem</MedlineTA><NlmUniqueID>101240303</NlmUniqueID><ISSNLinking>1573-4064</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000970">Antineoplastic Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000998">Antiviral Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D047188">Chalcones</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName UI="D000970" MajorTopicYN="N">Antineoplastic Agents</DescriptorName><QualifierName UI="Q000737" MajorTopicYN="Y">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D000998" MajorTopicYN="N">Antiviral Agents</DescriptorName><QualifierName UI="Q000737" MajorTopicYN="Y">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D045744" MajorTopicYN="N">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D047188" MajorTopicYN="N">Chalcones</DescriptorName><QualifierName UI="Q000737" MajorTopicYN="Y">chemistry</QualifierName><QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D004353" MajorTopicYN="N">Drug Evaluation, Preclinical</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D014780" MajorTopicYN="N">Viruses</DescriptorName><QualifierName UI="Q000187" MajorTopicYN="Y">drug effects</QualifierName></MeshHeading></MeshHeadingList><KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="N">Anticancer</Keyword><Keyword MajorTopicYN="N">antiviral</Keyword><Keyword MajorTopicYN="N">aryl/heteroaryl</Keyword><Keyword MajorTopicYN="N">colon</Keyword><Keyword MajorTopicYN="N">structure-activity relationship</Keyword><Keyword MajorTopicYN="N">thienyl chalcone.</Keyword></KeywordList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2017</Year><Month>12</Month><Day>02</Day></PubMedPubDate><PubMedPubDate PubStatus="revised"><Year>2018</Year><Month>04</Month><Day>28</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2018</Year><Month>04</Month><Day>29</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2018</Year><Month>5</Month><Day>25</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2019</Year><Month>3</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2018</Year><Month>5</Month><Day>25</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">29792154</ArticleId><ArticleId IdType="pii">MC-EPUB-90639</ArticleId><ArticleId IdType="doi">10.2174/1573406414666180524074648</ArticleId></ArticleIdList></PubmedData></pubmed><affiliations><list><country><li>Inde</li><li>États-Unis</li></country><region><li>Illinois</li><li>Texas</li></region></list><tree><country name="Inde"><noRegion><name sortKey="Patil, Vikrant" sort="Patil, Vikrant" uniqKey="Patil V" first="Vikrant" last="Patil">Vikrant Patil</name></noRegion><name sortKey="Patil, Siddappa A" sort="Patil, Siddappa A" uniqKey="Patil S" first="Siddappa A" last="Patil">Siddappa A. Patil</name></country><country name="États-Unis"><region name="Illinois"><name sortKey="Patil, Renukadevi" sort="Patil, Renukadevi" uniqKey="Patil R" first="Renukadevi" last="Patil">Renukadevi Patil</name></region><name sortKey="Beaman, Kenneth" sort="Beaman, Kenneth" uniqKey="Beaman K" first="Kenneth" last="Beaman">Kenneth Beaman</name><name sortKey="Bugarin, Alejandro" sort="Bugarin, Alejandro" uniqKey="Bugarin A" first="Alejandro" last="Bugarin">Alejandro Bugarin</name><name sortKey="Patil, Shivaputra A" sort="Patil, Shivaputra A" uniqKey="Patil S" first="Shivaputra A" last="Patil">Shivaputra A. Patil</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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