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Article: Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors

TitleDesign, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors
Authors
KeywordsMolecular modeling
Antiviral
Inhibitor
HIV-1 Tat-TAR
Quinoline derivatives
Issue Date2009
Citation
Bioorganic and Medicinal Chemistry, 2009, v. 17, n. 5, p. 1948-1956 How to Cite?
AbstractThirty-two quinoline derivatives were designed and synthesized as HIV-1 Tat-TAR interaction inhibitors. All the compounds showed high antiviral activities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Nine of them with low cytotoxicities were evaluated by Tat dependent HIV-1 LTR-driven CAT gene expression colorimetric enzyme assay in human 293T cells, indicating effective inhibitory activities of blocking the Tat-TAR interaction. Molecular modeling experiments indicated that these compounds may inhibit Tat-TAR interaction by binding to Tat protein instead of TAR RNA. © 2009 Elsevier Ltd. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/297368
ISSN
2020 Impact Factor: 3.641
2020 SCImago Journal Rankings: 0.721
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorChen, Shuguang-
dc.contributor.authorChen, Ran-
dc.contributor.authorHe, Meizi-
dc.contributor.authorPang, Ruifang-
dc.contributor.authorTan, Zhiwu-
dc.contributor.authorYang, Ming-
dc.date.accessioned2021-03-15T07:33:37Z-
dc.date.available2021-03-15T07:33:37Z-
dc.date.issued2009-
dc.identifier.citationBioorganic and Medicinal Chemistry, 2009, v. 17, n. 5, p. 1948-1956-
dc.identifier.issn0968-0896-
dc.identifier.urihttp://hdl.handle.net/10722/297368-
dc.description.abstractThirty-two quinoline derivatives were designed and synthesized as HIV-1 Tat-TAR interaction inhibitors. All the compounds showed high antiviral activities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Nine of them with low cytotoxicities were evaluated by Tat dependent HIV-1 LTR-driven CAT gene expression colorimetric enzyme assay in human 293T cells, indicating effective inhibitory activities of blocking the Tat-TAR interaction. Molecular modeling experiments indicated that these compounds may inhibit Tat-TAR interaction by binding to Tat protein instead of TAR RNA. © 2009 Elsevier Ltd. All rights reserved.-
dc.languageeng-
dc.relation.ispartofBioorganic and Medicinal Chemistry-
dc.subjectMolecular modeling-
dc.subjectAntiviral-
dc.subjectInhibitor-
dc.subjectHIV-1 Tat-TAR-
dc.subjectQuinoline derivatives-
dc.titleDesign, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors-
dc.typeArticle-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.bmc.2009.01.038-
dc.identifier.pmid19217787-
dc.identifier.scopuseid_2-s2.0-61349138873-
dc.identifier.volume17-
dc.identifier.issue5-
dc.identifier.spage1948-
dc.identifier.epage1956-
dc.identifier.isiWOS:000264067900021-
dc.identifier.issnl0968-0896-

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