HYDROPHOBIC CIS-PLATINUM COMPLEXES EFFICIENTLY INCORPORATED INTO LIPOSOMES

摘要

The present invention concerns a platinum (II) four-coordinant complex having formula (I), wherein R1 is an alkyl diamine or cycloalkyl diamine and R2 and R3 are an alkylcarboxylato containing from five to ten carbon atoms. The R1 is preferably trans-D,L-1,2-diaminocyclohexane, trans-R,R-1,2-diaminocyclohexane, trans-S,S-1,2-diaminocyclohexane, cis-1,2-diaminocylohexane ethylene diamine or 1,1-bis(aminomethyl)cyclohexane. In a further aspect, the present invention involves preparation and therapeutic use of a liposome comprising a phospholipid and a four-coordinate platinum complex having formula (II), wherein R1 is an alkyl diamine or cycloalkyl diamine and R2 and R3 are an alkylcarboxylato containing from about five to about fourteen carbon atoms.