N. Garelli et al., CYTOTOXIC ACTIVITY OF NEW AMPHIPHILIC PERFLUOROALKYLATED BIPYRIDINE PLATINUM AND PALLADIUM COMPLEXES INCORPORATED INTO LIPOSOMES, European journal of medicinal chemistry, 28(3), 1993, pp. 235-242
The in vitro cytotoxic activity of 13 new perfluoroalkylated side-chai
n bipyridine Pt and Pd complexes, besides their hydrocarbon analogs, w
hen incorporated into liposomes, has been assessed against a human hea
d and neck carcinoma cell line (CAL 27) sensitive to CDDP. All the lip
osome-entrapped complexes showed an inhibition of the cellular growth
(IC50 values from 5-154 muM and from 2-84 muM for respectively 5 h and
69 h of exposure). The most effective ones, 2 palladium complexes, ha
d an IC50 (5 and 10 muM for 5 h exposure) close to that of unencapsula
ted CDDP (4 muM). Most importantly, our results show that the presence
of perfluoroalkylated tails, which confers fluorophilicity and lipoph
obicity on the complexes, does not impair their cytotoxic activity.