Platinum compounds based on propane-1,3-diamine derivatives for treating carcinomas that are resistant to cis-platin, induce apoptosis but not by activation of caspase

摘要

Platinum(II) compounds (A1)-(A3) for treatment of resistant carcinoma. Platinum(II) compounds of formulae (A1)-(A3) for treatment of resistant carcinoma R : tetrahydropyran-2-oxy, cyclohexyloxy or Me; n : 2-16 . An independent claim is included for a method for increasing the solubility of (A1)-(A3) by addition of mixed micelles and/or cylodextrins in polar solvents. [Image] ACTIVITY : Cytostatic. The compound THP ((A2) with n = 11; R not stated) was tested against the cell line 1411HP, resistant to cis-platin (cP) in a 2 hour contact test. At a concentration of 3 mu M viability was reduced to zero while a concentration of 1 mu M reduced viability to about 85%. The concentration of cP required for zero viability was 100 mu M. MECHANISM OF ACTION : Induction of apoptosis by a mechanism that is not based on activation of caspases (contrast cis-platin).