HER2 inhibition efficiency of 6-amino-2-methyl-2-phenethyl-2H-benzopyran and feasibility of the 64Cu-labeled benzopyran derivative in cancer diagnosis

Abstract

A series of benzopyran derivatives were synthesised, and the target product, 6-amino-2-methyl-2-phenethyl-2H-benzopyran (compound 4), was labeled with radioactive ⁶⁴Cu (⁶⁴Cu-6). Compound 4 induced significant apoptosis and suppressed cell proliferation of SK-BR-3 by inhibiting overexpression of the HER2 protein. Furthermore, the ⁶⁴Cu-6 with significant stability and lipophilicity showed high cellular uptake and cytotoxicity in SK-BR-3, suggesting its promise for dual applications, namely as a diagnostic imaging probe in positron emission tomography (PET) and in cancer treatment.