BO-653

BO-653 is a synthetic lipophilic antioxidant developed as a drug candidate for the inhibition of lipid peroxidation in vivo. Its structure is based on a benzofuran core with di-tert-butyl and dipentyl substituents that enhance its hydrogen donor activity and hydrophobicity. BO-653 exhibits high affinity for low-density lipoprotein (LDL) and distributes well in vascular tissues. It has demonstrated potent inhibition of LDL oxidation—more effective than probucol or α-tocopherol—and suppresses lipid peroxide generation by both copper ion and lipoxygenase pathways[8][6]. In preclinical studies, BO-653 showed antiatherogenic effects in animal models by inhibiting LDL degradation by macrophages[8]. Clinically, it was investigated for the prevention of restenosis after angioplasty and for the treatment of atherosclerosis[4]. Additionally, BO-653 has shown antiviral activity against hepatitis C virus (HCV) replication in vitro and in chimeric mice with human hepatocytes; its antioxidant properties are integral to this effect[3][5]. The compound was initially developed by Chugai Pharmaceutical (a subsidiary of Roche), but development appears to have been discontinued[3].

Other names

2,3-dihydro-5-hydroxy-2,2-dipentyl-4,6-di-tert-butylbenzofuran