HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure–activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.

中文翻译：

---

(S)-1-(1-(咪唑并[1,2-a]吡啶-6-基)乙基)-6-(1-甲基-1H-吡唑-4-基)-1H-[1, 2,3]三唑并[4,5-b]吡嗪（沃利替尼）作为癌症治疗临床开发中的高效选择性间充质-上皮转化因子（c-Met）抑制剂

HGF/c-Met 信号传导与人类癌症有关。在此，我们描述了一系列新型三唑并吡嗪 c-Met 抑制剂的发明。研究了这些化合物的构效关系，从而鉴定出化合物28，该化合物在小鼠体内表现出良好的药代动力学特性，在无胸腺裸鼠的人神经胶质瘤异种移植模型中表现出良好的抗肿瘤活性。