Cis-dichloro-platinum peptide complexes - for use as cytostatics, antimicrobials, antivirals and immunosuppressants

摘要

New Pt peptide complexes are of formula (Cl)2Pt - NH2-CHR1CO- NHCR1CO -n NHCHR2COOR3 2. In the formula R1 and R2 are H or 1-4C alkyl opt. substd. by OH, NH2, MeO, EtO, SH, MeS, EtS or ArCH2; Ar is phenyl opt. substd. by OH, MeO or EtO; R3 is 1-4C alkyl; n = 0-3. Cpds. (I) have cytostatic, antimicrobial, antiviral and immunosuppressant activity, combined with much lower toxicity than cis- Pt(NH3)2CL2 (II). E.G. cis- PtCl2-(GlyGlyOEt)2 (Ia) has an LD50 of 405 mg/kg (mouse) compared with 12 mg/kg for (II). In an example, (Ia) is prepd. by reacting cis-PtCl2-(GlyOH)2 with p-nitrophenol and reacting the ester with GlyOEt.