Caffeine derived platinum(II) N-heterocyclic carbene complexes with multiple anti-cancer activities

Organometallic platinum(II) terpyridine complexes with a caffeine derived N-heterocyclic carbene (NHC) ligand were investigated as possible anti-cancer drugs in comparison to analogs, which contain N-coordinated theobromine. In general the carbene complexes displayed significantly higher biological activity than the theobromine analogs. In particular, the caffeine derived organometallic platinum(II) complex [PtII(2,20: 60,200-terpyridine) (1,3,7,9-tetramethylxanthine-8-ylidene)](PF6) 2 (1) displayed very promising cytotoxic activity towards several cancer cell lines, and showed in-vitro anti-angiogenic effects at sub-cytotoxic concentrations. Moreover, it induced neural differentiation-like morphological changes in breast adenocarcinoma (MCF-7) cells. (C) 2014 Elsevier B.V. All rights reserved.