A Cu(II) complex, that is, [Cu(CNC-B3)(IM-B7)](PF6)2, 1, containing CNC-B3 (L2) = CNC–pincer–vitamin B3 and IM-B7 (L3) = 1H-imidazole-1-methanamine-vitamin B7 conjugates, was developed as a potential chemotherapeutic agent for breast cancer cell lines. The Cu(II) complex brings about a remarkable in vitro cytotoxicity in comparison with cisplatin and tamoxifen against MDA-MB-231 and MCF-7 cancer cell lines. Interestingly, the Cu(II) complex was considerably less toxic to MRC-5 normal cells.