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Conference Paper: Design, synthesis, and biological evaluation of novel substituted [1,2,3]triazolo[4,5-d]pyrimidines as HIV-1 Tat-TAR interaction inhibitors

TitleDesign, synthesis, and biological evaluation of novel substituted [1,2,3]triazolo[4,5-d]pyrimidines as HIV-1 Tat-TAR interaction inhibitors
Authors
KeywordsAntiviral activities
Heterocycle compounds
TAR RNA
Substituted purines
HIV
Tat-TAR inhibitors
Issue Date2010
Citation
Pure and Applied Chemistry, 2010, v. 82, n. 1, p. 339-347 How to Cite?
AbstractA novel series of compounds, derived from [1, 2, 3]triazolo[4, 5-d]pyrimidines with a guanidyl group or amino group-terminated side chain was designed and synthesized as HIV-1 trans-activator of transcription-trans- activation responsive region (Tat-TAR) interaction inhibitors. Their ability to inhibit Tat-TAR RNA interaction was determined by a Tat-dependent HIV-1 long terminal repeat (LTR)-driven chloramphenicol acetyltransferase (CAT) assay and simian immunodeficiency virus (SIV)-induced syncytium evaluation. The binding of the compounds with TAR RNA was conducted by molecular modeling and capillary electrophoresis (CE) analysis. The results showed that all the compounds could block the Tat-TAR interaction and have antiviral activities. © 2010 IUPAC.
Persistent Identifierhttp://hdl.handle.net/10722/297303
ISSN
2020 Impact Factor: 2.453
2020 SCImago Journal Rankings: 0.439
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorYu, Fei-
dc.contributor.authorPang, Ruifang-
dc.contributor.authorYuan, Dekai-
dc.contributor.authorHe, Meizi-
dc.contributor.authorZhang, Chunlei-
dc.contributor.authorChen, Shuguang-
dc.contributor.authorYang, Ming-
dc.date.accessioned2021-03-15T07:33:28Z-
dc.date.available2021-03-15T07:33:28Z-
dc.date.issued2010-
dc.identifier.citationPure and Applied Chemistry, 2010, v. 82, n. 1, p. 339-347-
dc.identifier.issn0033-4545-
dc.identifier.urihttp://hdl.handle.net/10722/297303-
dc.description.abstractA novel series of compounds, derived from [1, 2, 3]triazolo[4, 5-d]pyrimidines with a guanidyl group or amino group-terminated side chain was designed and synthesized as HIV-1 trans-activator of transcription-trans- activation responsive region (Tat-TAR) interaction inhibitors. Their ability to inhibit Tat-TAR RNA interaction was determined by a Tat-dependent HIV-1 long terminal repeat (LTR)-driven chloramphenicol acetyltransferase (CAT) assay and simian immunodeficiency virus (SIV)-induced syncytium evaluation. The binding of the compounds with TAR RNA was conducted by molecular modeling and capillary electrophoresis (CE) analysis. The results showed that all the compounds could block the Tat-TAR interaction and have antiviral activities. © 2010 IUPAC.-
dc.languageeng-
dc.relation.ispartofPure and Applied Chemistry-
dc.subjectAntiviral activities-
dc.subjectHeterocycle compounds-
dc.subjectTAR RNA-
dc.subjectSubstituted purines-
dc.subjectHIV-
dc.subjectTat-TAR inhibitors-
dc.titleDesign, synthesis, and biological evaluation of novel substituted [1,2,3]triazolo[4,5-d]pyrimidines as HIV-1 Tat-TAR interaction inhibitors-
dc.typeConference_Paper-
dc.description.naturelink_to_OA_fulltext-
dc.identifier.doi10.1351/PAC-CON-09-01-04-
dc.identifier.scopuseid_2-s2.0-76049109973-
dc.identifier.volume82-
dc.identifier.issue1-
dc.identifier.spage339-
dc.identifier.epage347-
dc.identifier.eissn1365-3075-
dc.identifier.isiWOS:000274709300030-
dc.identifier.issnl0033-4545-

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