Structure–activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-α production and T Cell proliferation

…, M Matsumoto, F Obara, T Nagasaki, H Hayashi

文献索引：Tobe, Masanori; Isobe, Yoshiaki; Tomizawa, Hideyuki; Matsumoto, Mitsuhiro; Obara, Fumihiro; Nagasaki, Takahiro; Hayashi, Hideya Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 545 - 548

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被引用次数: 19

摘要

We synthesized 4-chlorophenethylaminoquinazoline derivatives and evaluated their inhibitory activities toward both TNF-α production and T cell proliferation responses. Compound 2f, containing a piperazine ring at the C (7)-position of the quinazoline ring, exhibited more potent inhibitory activities toward both than the lead compound 1a. A smaller N-substituent in the piperazine ring was required for inhibition of TNF-α production.