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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.
Afiliación
  • Shad MS; Department of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, Belgium.
  • Claes S; Laboratory 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, Belgium.
  • Goffin E; Department of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, Belgium.
  • Van Loy T; Laboratory 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, Belgium.
  • Schols D; Laboratory 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, Belgium.
  • De Jonghe S; Laboratory 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, Belgium.
  • Dehaen W; Department of Chemistry, Molecular Design and Synthesis, KU Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Leuven, Belgium.
Molecules ; 26(20)2021 Oct 18.
Article en En | MEDLINE | ID: mdl-34684878
ABSTRACT
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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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Infecciones por VIH / VIH / Fármacos Anti-VIH / Receptores CXCR4 / Isoquinolinas Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Bélgica
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Infecciones por VIH / VIH / Fármacos Anti-VIH / Receptores CXCR4 / Isoquinolinas Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Bélgica