Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties

YesimA. Tahirovic; Valarie M. Truax; Robert J. Wilson; Edgars Jecs; Huy H. Nguyen; Eric J. Miller; Michelle B. Kim; Katie M. Kuo; Tao Wang; Chi S. Sum; Mary E. Cvijic; Gretchen M. Schroeder; Lawrence J. Wilson; Dennis C. Liotta

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Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties

机译：发现 n -alkyl piperazine侧链的CXCR4拮抗剂，具有改善的药物状性质

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机译：<！[CDATA [CDATA [一种与哌啶基和哌嗪基烷基胺侧链的新型CXCR4拮抗剂，设计为丁胺替换。这些化合物中的几种在SDF-1诱导的钙通量测定中显示出与母体化合物TIQ-15（ 5）的相似活性。初步结构 - 活性关系研究导致我们鉴定含有在毒蕈碱乙酰胆碱受体（MACHR）钙通量测定中的改善的偏离目标效果的含有含有 N-丙基哌嗪侧链类似物的系列载体。有限的药物安全面板屏幕。进一步促进SAR和优化药物性质的努力导致了鉴定 N'-乙基 - N-丙基 - 哌嗪四氢异喹啉衍生物 44和N-丙基 - 哌嗪苯并咪唑化合物< B> 37，其在没有MACHR或CYP450抑制的最佳整体型材，PAMPA测定中的良好渗透性和人肝微粒体中的代谢稳定性。]> 展开▼

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《ACS medicinal chemistry letters》 |2018年第5期|共6页

作者
YesimA. Tahirovic; Valarie M. Truax; Robert J. Wilson; Edgars Jecs; Huy H. Nguyen; Eric J. Miller; Michelle B. Kim; Katie M. Kuo; Tao Wang; Chi S. Sum; Mary E. Cvijic; Gretchen M. Schroeder; Lawrence J. Wilson; Dennis C. Liotta;
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Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Bristol-Myers Squibb R&

D US Route 206 and Province Line Road Princeton New Jersey 08543-4000 United States;

Bristol-Myers Squibb R&

D US Route 206 and Province Line Road Princeton New Jersey 08543-4000 United States;

Bristol-Myers Squibb R&

D US Route 206 and Province Line Road Princeton New Jersey 08543-4000 United States;

Bristol-Myers Squibb R&

D US Route 206 and Province Line Road Princeton New Jersey 08543-4000 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

Department of Chemistry Emory University 1515 Dickey Drive Atlanta Georgia 30322 United States;

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正文语种 eng

中图分类药学;化学;

关键词
calcium flux; CXCR4 antagonists; CXCR4 receptor; CYP450; liver microsomes; muscarinic receptor; PAMPA; piperazine; tetrahydroisoquinoline;

机译：钙通量;CXCR4拮抗剂;CXCR4受体;CYP450;肝微粒体;毒蕈碱受体;PAMPA;哌嗪;四氢异喹啉;

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1. Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties [J] . YesimA. Tahirovic, Valarie M. Truax, Robert J. Wilson, ACS medicinal chemistry letters . 2018,第5期

机译：发现 n -alkyl piperazine侧链的CXCR4拮抗剂，具有改善的药物状性质

2. Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties [J] . Eric J. Miller, Edgars Jecs, Valarie M. Truax, Journal of Medicinal Chemistry . 2018,第3期

机译：发现含四羟基喹啉的CXCR4拮抗剂，具有改善的体外探险性能

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机译：发现有效和选择性FLT3抑制剂（Z）-N-（5 - （（5-氟-2-氧代吲哚-3- ylidene）甲基）-4-甲基-1H-吡咯-3-Y1）-3-（ Pyrrolidin-1-yl）丙酰胺，具有改善的药物状性质和FLT3-ITD阳性急性髓性白血病的优异功效

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Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties

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