Design, synthesis and in vitro cytotoxicity of a cis-dichloroplatinum (II) complex linked to the minor groove binder stallimycin.
Two potentially hydrophilic platinum (II) complexes 10 and 11 bound to the minor groove binder stallimycin (distamycin A, CAS 636-47-5) by L-cysteine and D,L-2,3-diaminopropionic acid have been synthesized. The in vitro cytotoxicity of both these complexes was evaluated against several cell lines. None of the synthesized platinum complexes showed greater activity than that of cisplatin (cis-DDP, 1) (CAS 15663-27-1). Interestingly, the free ligands 6 and 9 were more active than the related platinum complexes 10 and 11, respectively, with respect to RAJI, CCRF-CEM and MOLT-4 human leukaemia cell lines.
Baraldi
Pier Giovanni
PG
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy. pgb@dns.unife.it
Tabrizi
Mojgan Aghazadeh
MA
Pavani
Maria Giovanna
MG
Nuñez
Maria del Carmen
Mdel C
Makaeva
Rimma
R
Gambari
Roberto
R
La Colla
Paolo
P
Romagnoli
Romeo
R
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002945:Cisplatin / Q000008:administration & dosage / Q000737:chemistry*; D003545:Cysteine / Q000737:chemistry; D004121:Dimethyl Sulfoxide; D004214:Distamycins / Q000008:administration & dosage / Q000737:chemistry*; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004214:Distamycins; D007202:Indicators and Reagents; C030000:stallimycin; D003545:Cysteine; D002945:Cisplatin; D004121:Dimethyl Sulfoxide