title: Design, synthesis and in vitro cytotoxicity of a cis-dichloroplatinum (II) complex linked to the minor groove binder stallimycin.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy. pgb@dns.unife.it
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Mojgan Aghazadeh
authors.initials: MA
authors.lastname: Tabrizi
authors.forename: Maria Giovanna
authors.initials: MG
authors.lastname: Pavani
authors.forename: Maria del Carmen
authors.initials: Mdel C
authors.lastname: Nuñez
authors.forename: Rimma
authors.initials: R
authors.lastname: Makaeva
authors.forename: Roberto
authors.initials: R
authors.lastname: Gambari
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D004214:Distamycins; D007202:Indicators and Reagents; C030000:stallimycin; D003545:Cysteine; D002945:Cisplatin; D004121:Dimethyl Sulfoxide