Title of article :
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors
Author/Authors :
Francis Beaulieu، نويسنده , , Carl Ouellet، نويسنده , , Edward H. Ruediger، نويسنده , , Makonen Belema، نويسنده , , Yuping Qiu، نويسنده , , Xuejie Yang، نويسنده , , Jacques Banville، نويسنده , , James R. Burke، نويسنده , , Kurt R. Gregor، نويسنده , , John F. MacMaster، نويسنده , , Alain Martel، نويسنده , , Kim W. McIntyre، نويسنده , , Mark A. Pattoli، نويسنده , , F. Christopher Zusi، نويسنده , , Dolatrai Vyas، نويسنده ,
Abstract :
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 μM), which however was considerably less potent against IKK-1 (IC50 = 4.0 μM). In order to further explore the SAR around the imidazoquinoxaline tricyclic structure of 1, we prepared a series of tetracyclic analogues (7, 13, and 18). The synthesis and biological activities of these potent IKK inhibitors are described.
Keywords :
IKK inhibitors , NF-?B , TNF-? , Quinoxaline
