Discovery of potent CCR4 antagonists: synthesis and structure–activity relationship study of 2, 4-diaminoquinazolines

K Yokoyama, N Ishikawa, S Igarashi, N Kawano…

文献索引：Yokoyama, Kazuhiro; Ishikawa, Noriko; Igarashi, Susumu; Kawano, Noriyuki; Hattori, Kazuyuki; Miyazaki, Takahiro; Ogino, Shin-ichi; Matsumoto, Yuzo; Takeuchi, Makoto; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 7021 - 7032

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被引用次数: 27

摘要

A new series of quinazolines that function as CCR4 antagonists were discovered during the screening of our corporate compound libraries. Subsequent compound optimization elucidated the structure–activity relationships and led the identification of 2-(1, 4′- bipiperidine-1′-yl)-N-cycloheptyl-6, 7-dimethoxyquinazolin-4-amine 14a, which showed potent inhibition in the [35S] GTPγS-binding assay (IC50= 18nM). This compound also ...