Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation

…, Y Isobe, H Tomizawa, T Nagasaki, H Takahashi…

Index: Tobe, Masanori; Isobe, Yoshiaki; Tomizawa, Hideyuki; Nagasaki, Takahiro; Takahashi, Hirotada; Fukazawa, Tominaga; Hayashi, Hideya Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 3 p. 383 - 391

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Citation Number: 123

Abstract

We disclose here a new structural class of low-molecular-weight inhibitors of NF-κB activation that were designed and synthesized by starting from quinazoline derivative 6a. Structure–activity relationship (SAR) studies based on 6a elucidated the structural requirements essential for the inhibitory activity toward NF-κB transcriptional activation, and led to the identification of the 6-amino-4-phenethylaminoquinazoline skeleton as the basic ...