jm501662b_si_003.pdf (4.59 MB)
Dual Antitumor and Antiangiogenic Activity of Organoplatinum(II) Complexes
journal contribution
posted on 2015-12-17, 07:17 authored by Ana Zamora, Sergio
A. Pérez, Venancio Rodríguez, Christoph Janiak, Gorakh S. Yellol, José RuizA library of over 20 cycloplatinated
compounds of the type [Pt(dmba-R)LCl]
(dmba-R = C,N-dimethylbenzylamine-like ligand; R being MeO, Me, H,
Br, F, CF3, and NO2 substituents in the R5 or R4 position of the phenyl ring; L = DMSO and
P(C6H4CF3-p)3) has been
prepared. All compounds are active in both human ovarian carcinoma
A2780 cells and cisplatin-resistant A2780cisR cells, with most of
the DMSO platinum complexes exhibiting IC50 values in the
submicromolar range in the A2780 cell line. Interestingly, DMSO platinum
complexes show low cytotoxicity in the nontumorigenic kidney cell
line BGM and therefore high selectivity factors SF. In addition, some
of the DMSO platinum complexes effectively inhibit angiogenesis in
the human umbilical vein endothelial cell line EA.hy926. These are
the first platinum(II) complexes reported to inhibit angiogenesis
at a close concentration to their IC50 in A2780 cells,
turning them into dual cytotoxic and antiangiogenic compounds.