2. Academic Validation
  3. A novel structural class of potent inhibitors of NF-kappa B activation: structure-activity relationships and biological effects of 6-aminoquinazoline derivatives

A novel structural class of potent inhibitors of NF-kappa B activation: structure-activity relationships and biological effects of 6-aminoquinazoline derivatives

  • Bioorg Med Chem. 2003 Sep 1;11(18):3869-78. doi: 10.1016/s0968-0896(03)00438-3.
Masanori Tobe 1,  Yoshiaki Isobe,  Hideyuki Tomizawa,  Takahiro Nagasaki,  Hirotada Takahashi,  Hideya Hayashi
Affiliations

Affiliation

  • 1 Research Division, Sumitomo Pharmaceuticals Co., Ltd., 1-98 Kasugade Naka 3-Chome, Konohana-ku, Osaka 554-0022, Japan.
PMID: 12927847 DOI: 10.1016/s0968-0896(03)00438-3
Abstract

In this study, we have investigated the roles of substituents on the terminal phenyl ring at the C(4)-position of the quinazoline core to complete the structure-activity relationships (SARs) of our NF-kappa B activation inhibitors. Among them, compound 12j afforded highly potent inhibitory activity toward NF-kappa B transcriptional activation with IC(50) value of 2 nM, along with an excellent in vivo efficacy by reducing the edema formation seen in carrageenin-induced inflammation of the rat hind paw.

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