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- Publisher Website: 10.1016/j.bmc.2009.01.038
- Scopus: eid_2-s2.0-61349138873
- PMID: 19217787
- WOS: WOS:000264067900021
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Article: Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors
Title | Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors |
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Authors | |
Keywords | Molecular modeling Antiviral Inhibitor HIV-1 Tat-TAR Quinoline derivatives |
Issue Date | 2009 |
Citation | Bioorganic and Medicinal Chemistry, 2009, v. 17, n. 5, p. 1948-1956 How to Cite? |
Abstract | Thirty-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 Identifier | http://hdl.handle.net/10722/297368 |
ISSN | 2023 Impact Factor: 3.3 2023 SCImago Journal Rankings: 0.614 |
ISI Accession Number ID |
DC Field | Value | Language |
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dc.contributor.author | Chen, Shuguang | - |
dc.contributor.author | Chen, Ran | - |
dc.contributor.author | He, Meizi | - |
dc.contributor.author | Pang, Ruifang | - |
dc.contributor.author | Tan, Zhiwu | - |
dc.contributor.author | Yang, Ming | - |
dc.date.accessioned | 2021-03-15T07:33:37Z | - |
dc.date.available | 2021-03-15T07:33:37Z | - |
dc.date.issued | 2009 | - |
dc.identifier.citation | Bioorganic and Medicinal Chemistry, 2009, v. 17, n. 5, p. 1948-1956 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/10722/297368 | - |
dc.description.abstract | Thirty-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.language | eng | - |
dc.relation.ispartof | Bioorganic and Medicinal Chemistry | - |
dc.subject | Molecular modeling | - |
dc.subject | Antiviral | - |
dc.subject | Inhibitor | - |
dc.subject | HIV-1 Tat-TAR | - |
dc.subject | Quinoline derivatives | - |
dc.title | Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors | - |
dc.type | Article | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.bmc.2009.01.038 | - |
dc.identifier.pmid | 19217787 | - |
dc.identifier.scopus | eid_2-s2.0-61349138873 | - |
dc.identifier.volume | 17 | - |
dc.identifier.issue | 5 | - |
dc.identifier.spage | 1948 | - |
dc.identifier.epage | 1956 | - |
dc.identifier.isi | WOS:000264067900021 | - |
dc.identifier.issnl | 0968-0896 | - |