CYTOTOXIC ACTIVITY OF NEW AMPHIPHILIC PERFLUOROALKYLATED BIPYRIDINE PLATINUM AND PALLADIUM COMPLEXES INCORPORATED INTO LIPOSOMES

Citation
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
Citations number
36
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
28
Issue
3
Year of publication
1993
Pages
235 - 242
Database
ISI
SICI code
0223-5234(1993)28:3<235:CAONAP>2.0.ZU;2-F
Abstract
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.