In our efforts to discover novel inhibitors of Wnt/β-catenin signaling, we have identified a structurally related series of quinazolines as potent inhibitors in colorectal cancer cells harboring mutations in CTNNB1 or APC. Although a few quinazoline analogs have been reported in the literature as inhibitors of the Wnt/β-catenin signaling pathway [16-19], the set of compounds that we have identified is structurally distinct. Here, CTNNB1 is linked to colorectal cancer.