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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| Format: | Article |
| Language: | English |
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MDPI AG
2021-10-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/20/6297 |
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| author | Mastaneh Safarnejad Shad Sandra Claes Eline Goffin Tom Van Loy Dominique Schols Steven De Jonghe Wim Dehaen |
| author_facet | Mastaneh Safarnejad Shad Sandra Claes Eline Goffin Tom Van Loy Dominique Schols Steven De Jonghe Wim Dehaen |
| author_sort | Mastaneh Safarnejad Shad |
| collection | DOAJ |
| 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 <b>24c</b> being the most promising one, since it displayed consistently low nanomolar activity in the various assays. |
| first_indexed | 2024-03-10T06:20:19Z |
| format | Article |
| id | doaj.art-987ef9297c144093a160c41d8fc60881 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T06:20:19Z |
| publishDate | 2021-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-987ef9297c144093a160c41d8fc608812023-11-22T19:21:08ZengMDPI AGMolecules1420-30492021-10-012620629710.3390/molecules26206297Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 AntagonistsMastaneh Safarnejad Shad0Sandra Claes1Eline Goffin2Tom Van Loy3Dominique Schols4Steven De Jonghe5Wim Dehaen6Department of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, BelgiumLaboratory of Virology and Chemotherapy, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumDepartment of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, BelgiumLaboratory of Virology and Chemotherapy, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumLaboratory of Virology and Chemotherapy, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumLaboratory of Virology and Chemotherapy, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumDepartment of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, BelgiumAn 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 <b>24c</b> being the most promising one, since it displayed consistently low nanomolar activity in the various assays.https://www.mdpi.com/1420-3049/26/20/6297isoquinolineCXCR4 antagonistHIV |
| spellingShingle | Mastaneh Safarnejad Shad Sandra Claes Eline Goffin Tom Van Loy Dominique Schols Steven De Jonghe Wim Dehaen Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists Molecules isoquinoline CXCR4 antagonist HIV |
| 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 | isoquinoline CXCR4 antagonist HIV |
| url | https://www.mdpi.com/1420-3049/26/20/6297 |
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