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The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2007 Nov 1 , DOI: 10.1016/j.bmcl.2007.07.104
R. Graham Robinett , Alex J. Freemerman , Michael A. Skinner , Lisa Shewchuk , Karen Lackey

Substituted 4-(3-hydroxyanilino)-quinoline compounds, initially identified as small-molecule inhibitors of src family kinases, have been evaluated as potential inhibitors of RET kinase. Three compounds, 38, 31, and 40, had K(i)'s of 3, 25, and 50 nM in an in vitro kinase assay; while a cell based kinase assay showed K(i)'s of 300, 100, and 45 nM, respectively. These compounds represent potential new leads for the treatment of medullary and papillary thyroid cancer.

中文翻译:

取代的4-(3-羟基苯胺基)-喹啉作为有效的RET激酶抑制剂的发现。

最初被鉴定为src家族激酶的小分子抑制剂的取代的4-(3-羟基苯胺基)-喹啉化合物已被评估为RET激酶的潜在抑制剂。在体外激酶测定中,三种化合物38、31和40的K(i)分别为3、25和50 nM。而基于细胞的激酶测定表明K(i)分别为300、100和45 nM。这些化合物代表了治疗甲状腺髓样和乳头状癌的潜在新线索。
更新日期:2017-01-31
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