A series of 2-oxo-1,2-dihydroquinoline-containing c-Met inhibitors were designed, synthesized and evaluated for their in vitro activities targeting c-Met. Most compounds showed high potency against c-Met with IC₅₀ values in the single-digit nM range. Among these compounds, two target compounds, namely 1h and 1n, stood out as the most potent c-Met inhibitors with IC₅₀s of 0.6 and 0.7nM, respectively. And 1a exhibited higher potency than BMS-777607 did with respect to the inhibition of cell proliferation. The introduction of electron-donating substituent was favorable for the activities of the compounds to some extent. Furthermore, molecular docking studies also gave encouraging results that supported this work.

中文翻译：

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设计，合成和生物学评估的c-Met激酶抑制剂带有2-氧-1,2-二氢喹啉支架

设计，合成和评估了一系列含有2-氧代-1,2-二氢喹啉的c-Met抑制剂，并评估了它们针对c-Met的体外活性。大多数化合物显示出对c-Met的高效力，IC ₅₀值在个位数nM范围内。在这些化合物中，两种目标化合物，即1h和1n，是最有效的c-Met抑制剂，IC ₅₀分别为0.6和0.7nM。1a在抑制细胞增殖方面比BMS-777607表现出更高的效力。给电子取代基的引入在某种程度上有利于化合物的活性。此外，分子对接研究也给出了令人鼓舞的结果，为这项工作提供了支持。