The design and synthesis of novel orally active inhibitors of AP-1 and NF-κB mediated transcriptional activation. SAR of in vitro and in vivo studies

…, BL Bennett, A Manning, L Ransone, C Spooner…

文献索引：Palanki, Moorthy S. S.; Erdman, Paul E.; Ren, Minghuan; Suto, Mark; Bennett, Brydon L.; Manning, Anthony; Ransone, Lynn; Spooner, Cheryl; Desai, Sonal; Ow, Arnie; Totsuka, Ryuichi; Tsao, Peter; Toriumi, Wataru Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 22 p. 4077 - 4080

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被引用次数: 33

摘要

We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF- κB mediated transcriptional activation. Among the derivatives prepared, 1-[2-(2-thienyl) quinazolin-4-ylamino]-3-methyl-3-pyrroline-2, 5-dione (10) showed significant activity in an adjuvant-induced arthritis rat model by reducing the swelling by 65% in the non-injected foot. The synthesis, structure–activity relationship, and in vivo activity are described.

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