Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains

[Image: see text] A structure–activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhibitor (IC(50) = 33 nM in CX...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Jecs, Edgars, Miller, Eric J., Wilson, Robert J., Nguyen, Huy H., Tahirovic, Yesim A., Katzman, Brook M., Truax, Valarie M., Kim, Michelle B., Kuo, Katie M., Wang, Tao, Sum, Chi S., Cvijic, Mary E., Schroeder, Gretchen M., Wilson, Lawrence J., Liotta, Dennis C.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2017
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5807867/
https://ncbi.nlm.nih.gov/pubmed/29456793
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00406
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