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Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.
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.
Afiliação
  • Jecs E; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Miller EJ; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Wilson RJ; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Nguyen HH; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Tahirovic YA; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Katzman BM; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Truax VM; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Kim MB; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Kuo KM; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Wang T; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States.
  • Sum CS; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States.
  • Cvijic ME; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States.
  • Schroeder GM; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States.
  • Wilson LJ; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
  • Liotta DC; Department of Chemistry, Emory University, 1515 Dickey Drive NE, Atlanta, Georgia 30322, United States.
ACS Med Chem Lett ; 9(2): 89-93, 2018 Feb 08.
Article em En | MEDLINE | ID: mdl-29456793
ABSTRACT
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 (IC50 = 33 nM in CXCL12-mediated Ca2+ flux) with enhanced stability in liver microsomes and reduced inhibition of CYP450 (2D6). The improved CXCR4 antagonist 15a has potential therapeutic application as a single agent or combinatory anticancer therapy.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article