Trans platinum complexes design: one novel water soluble oxime derivative that contains aliphatic amines in trans configuration.
In an attempt to design new antitumoral drugs based on transplatin complexes, we determined the experimental conditions for the preparation of trans-[Pt((CH(3))(2)CNOH)((CH(3))(2)CHNH(2))Cl(2)], and solved the crystal structure. The cytotoxicity of the novel complex, the cis counterpart, cisplatin, and a trans complex with aliphatic amines, as well as the capacity of some of these complexes to cause either apoptotic or necrotic cell death, was comparatively examined in NRK-52E rat renal tubular cells and HepG2 human hepatoma cells. The results indicate that the oxime complex with trans geometry, but not the one with cis geometry, causes death by apoptosis, making the complex potentially suitable for therapeutic purposes. However cytotoxicity values are higher in the case of cis geometry than in trans geometry in both tumoral and non-tumoral cell lines.
Quiroga
Adoración G
AG
Departamento de Química Inorgánica, Universidad Autónoma de Madrid, 28049 Madrid, Spain. adoracion.gomez@uam.es
Cubo
Leticia
L
de Blas
Elena
E
Aller
Patricio
P
Navarro-Ranninger
Carmen
C
D000588:Amines / Q000737:chemistry*; D000818:Animals; D002460:Cell Line; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D010091:Oximes / Q000737:chemistry*; D017671:Platinum Compounds / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D012995:Solubility; D013237:Stereoisomerism
D000588:Amines; D010091:Oximes; D017671:Platinum Compounds