Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription

2-[(7-Nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide was identified as a potent inhibitor of KIX-KID interaction from screening the NCI diversity set. Further structure-activity relationship studies identified 4-aniline substituted nitrobenzofurazans with improved selectivity.