SYNTHESIS AND BIOLOGICAL-ACTIVITY OF BINUCLEAR PLATINUM COMPLEXES CONTAINING 2 MONOFUNCTIONAL CIS-[PT(NH3)(2)CL](-DIPYRIDYL SELENIDES OR SULFIDES() UNITS BRIDGED BY 4,4')
Gh. Zhao et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF BINUCLEAR PLATINUM COMPLEXES CONTAINING 2 MONOFUNCTIONAL CIS-[PT(NH3)(2)CL](-DIPYRIDYL SELENIDES OR SULFIDES() UNITS BRIDGED BY 4,4'), Anti-cancer drug design (Print), 13(7), 1998, pp. 769-777
The synthesis of four binuclear platinum complexes of general formula
{cis-[Pt(NH3)(2)Cl](2)(L)} (NO3)(2) [L is 4,4'-dipyridyl sulfide (comp
ound I), 4,4'-dipyridyl selenide (compound II), bis(3-methyl-4-pyridyl
) sulfide (compound III) or bis(3-methyl-4-pyridyl) selenide (compound
IV)] has been achieved. These compounds have been characterized by el
emental analysis, IR, H-1-NMR, C-13-NMR and Pt-195-NMR spectroscopy. T
he above dinuclear platinum complexes have been assayed for antitumor
activity in vitro against the cisplatin-sensitive L1210 (the mice leuk
emia) and cisplatin-insensitive HCT8 (the human coloadenocarcinoma) ce
ll lines. The compounds show IC50 values comparable to or higher than
cisplatin against L1210 cell line; however, they have lower IC50 value
s than cisplatin against the cisplatin-insensitive HCT8 cell line. The
complexes containing S exhibit a cytotoxicity against the two cancer
cell lines superior to the Se analogues. DNA binding studies indicate
the compound I possibly interacts with DNA nonintercalatively. The mod
e of DNA binding of the dinuclear Pt(II) complexes bridged by 4,4'-dip
yridyl selenides or sulfides may be different to that of the aliphatic
diamine-bridged dinuclear Pt(II) complexes reported previously.