Author/Authors :
Moorthy S. S. Palanki، نويسنده , , Paul E. Erdman، نويسنده , , Minghuan Ren، نويسنده , , Mark Suto، نويسنده , , Brydon L. Bennett، نويسنده , , Anthony Manning، نويسنده , , Lynn Ransone، نويسنده , , Cheryl Spooner، نويسنده , , Sonal Desai، نويسنده , , Arnie Ow، نويسنده , , Ryuichi Totsuka، نويسنده , , Peter Tsao، نويسنده , , Wataru Toriumi، نويسنده ,
Abstract :
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.
