新型 2,3,4,5-四氢苯并[d]氮杂䓬衍生物为 2,4-二氨基嘧啶，是选择性的、口服生物利用度的 ALK 抑制剂，在 ALCL 小鼠模型中具有抗肿瘤疗效。
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
机构信息
Worldwide Discovery Research, Cephalon, Inc, 145 Brandywine Parkway, West Chester, PA 19380, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):463-6. doi: 10.1016/j.bmcl.2010.10.115. Epub 2010 Oct 27.
PMID:21074994
Abstract
The synthesis and biological evaluation of potent and selective anaplastic lymphoma kinase (ALK) inhibitors from a novel class of 2,4-diaminopyrimidines, incorporating 2,3,4,5-tetrahydro-benzo[d]azepine fragments, is described. An orally bioavailable analogue (18) that displayed antitumor efficacy in ALCL xenograft models in mice was identified and extensively profiled.
摘要
描述了一类新型的 2,4-二氨基嘧啶，其中包含 2,3,4,5-四氢苯并[d]氮杂卓片段，合成和生物评价其作为有效和选择性间变性淋巴瘤激酶（ALK）抑制剂的能力。鉴定出一种具有口服生物利用度的类似物（18），其在小鼠 ALCL 异种移植模型中显示出抗肿瘤功效，并对其进行了广泛的分析。
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