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Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Skerlj, Renato; Bridger, Gary; McEachern, Ernie; Harwig, Curtis; Smith, Chris; Wilson, Trevor; Veale, Duane; Yee, Helen; Crawford, Jason; Skupinska, Krystyna; Wauthy, Rossana; Yang, Wen; Zhu, Yongbao; Bogucki, David; Di Fluri, Maria; Langille, Jonathon; Huskens, Dana; De Clercq, Erik; Schols, Dominique.
Afiliación
  • Skerlj R; Genzyme Corp, 153 Second Avenue, Waltham, MA 02451, USA. renato.skerlj@genzyme.com
Bioorg Med Chem Lett ; 21(1): 262-6, 2011 Jan 01.
Article en En | MEDLINE | ID: mdl-21109432
An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Replicación Viral / VIH-1 / Fármacos Anti-VIH / Receptores CXCR4 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Replicación Viral / VIH-1 / Fármacos Anti-VIH / Receptores CXCR4 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: Estados Unidos