35982-14-0Relevant academic research and scientific papers
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
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
, p. 4077 - 4080 (2007/10/03)
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.
Quinazolines as cyclin dependent kinase inhibitors
Sielecki, Thais M.,Johnson, Tricia L.,Liu, Jie,Muckelbauer, Jodi K.,Grafstrom, Robert H.,Cox, Sarah,Boylan, John,Burton, Catherine R.,Chen, Haiying,Smallwood, Angela,Chang, Chong-Hwan,Boisclair, Michael,Benfield, Pamela A.,Trainor, George L.,Seitz, Steven P.
, p. 1157 - 1160 (2007/10/03)
Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined.
