Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists

An expansion of the structure–activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and ca...

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Autores principales: Shad, Mastaneh Safarnejad, Claes, Sandra, Goffin, Eline, Van Loy, Tom, Schols, Dominique, De Jonghe, Steven, Dehaen, Wim
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8539250/
https://www.ncbi.nlm.nih.gov/pubmed/34684878
http://dx.doi.org/10.3390/molecules26206297
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author Shad, Mastaneh Safarnejad
Claes, Sandra
Goffin, Eline
Van Loy, Tom
Schols, Dominique
De Jonghe, Steven
Dehaen, Wim
author_facet Shad, Mastaneh Safarnejad
Claes, Sandra
Goffin, Eline
Van Loy, Tom
Schols, Dominique
De Jonghe, Steven
Dehaen, Wim
author_sort Shad, Mastaneh Safarnejad
collection PubMed
description An expansion of the structure–activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and calcium mobilization assays, respectively. In addition, the anti-HIV activity of all analogues was determined. All compounds showed excellent activity, with compound 24c being the most promising one, since it displayed consistently low nanomolar activity in the various assays.
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spelling pubmed-85392502021-10-24 Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists Shad, Mastaneh Safarnejad Claes, Sandra Goffin, Eline Van Loy, Tom Schols, Dominique De Jonghe, Steven Dehaen, Wim Molecules Article An expansion of the structure–activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and calcium mobilization assays, respectively. In addition, the anti-HIV activity of all analogues was determined. All compounds showed excellent activity, with compound 24c being the most promising one, since it displayed consistently low nanomolar activity in the various assays. MDPI 2021-10-18 /pmc/articles/PMC8539250/ /pubmed/34684878 http://dx.doi.org/10.3390/molecules26206297 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Shad, Mastaneh Safarnejad
Claes, Sandra
Goffin, Eline
Van Loy, Tom
Schols, Dominique
De Jonghe, Steven
Dehaen, Wim
Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title_full Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title_fullStr Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title_full_unstemmed Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title_short Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists
title_sort synthesis and anti-hiv activity of a novel series of isoquinoline-based cxcr4 antagonists
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8539250/
https://www.ncbi.nlm.nih.gov/pubmed/34684878
http://dx.doi.org/10.3390/molecules26206297
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