A series of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives were designed, synthesized and evaluated for their biological activity. Most of these compounds showed potent activities against c-Met kinase and cell growth inhibition. The most promising compound, 7d, has the IC₅₀ values of 2.02 and 88 nM to inhibit c-Met kinase activity and cell growth in the MKN45 cell line, respectively. In addition, 7d is highly selective to c-Met and exhibits over 2500-fold selective inhibition to 16 tyrosine kinases evaluated.

中文翻译：

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[1,2,4]三唑并[3,4-b] [1,3,4]噻二唑衍生物的发现：新型，有效和选择性的c-Met激酶抑制剂：合成，SAR研究和生物学活性

设计，合成了一系列[1,2,4]三唑并[3,4-b] [1,3,4]噻二唑衍生物，并对其生物学活性进行了评估。这些化合物大多数显示出对c-Met激酶有效的活性和对细胞生长的抑制作用。最有前途的化合物7d的IC ₅₀值为2.02和88 nM，分别抑制c-Met激酶活性和MKN45细胞系中的细胞生长。此外，7d对c-Met具有高度选择性，对所评估的16种酪氨酸激酶表现出超过2500倍的选择性抑制。