title: Oxaliplatin analogues with carboxy derivatives of boldine with enhanced antioxidant activity.
abstract: A new oxaliplatin analog [Pt(dach)(L5)] (1) was synthesized and characterized as a continuation of a study of the previously reported [Pt(dach)(L6)] (2), where dach = (1R,2R)-diaminocyclohexane, L5 = 3-carboxyboldine, and L6 = 3-carboxypredicentrine. Compounds 1 and 2 exhibited a substantially enhanced antioxidant activity compared to oxaliplatin (130 and 30 times for 1 and 13 and 4 times for 2 using the DPPH and FRAP assays, resp.). In addition, 1 and 2 exhibited cytotoxic activity in the same range as oxaliplatin toward the two human tumor cell lines (MCF-7 and HT-29) studied and two to four times lower activity in the human colon nontumor cell line (CCD-841). Preadministration of L5 or L6 to the colon tumor (HT-29) and the colon nontumor (CCD-841) cell lines prior to oxaliplatin addition increased the viability of the nontumor cell line to a greater extent than that of the tumor cell line.
authors: Departamento de Química, Universidad Técnica Federico Santa María, Avenida España 1680, 2390123 Valparaíso, Chile.
authors: Marco
authors: M
authors: Mellado
authors: Centro de Investigaciones Biomédicas (CIB), Escuela de Medicina, Universidad de Valparaiso, Avenida Hontaneda 2664, 2340000 Valparaíso, Chile.
authors: Carlos
authors: C
authors: Jara
authors: Laboratorio de Investigación-Estrés Oxidativo, Escuela de Medicina, Universidad de Valparaiso, Avenida Brasil 1560, 2340000 Valparaíso, Chile.
authors: David
authors: D
authors: Astudillo
authors: Laboratorio de Investigación-Estrés Oxidativo, Escuela de Medicina, Universidad de Valparaiso, Avenida Brasil 1560, 2340000 Valparaíso, Chile.
authors: Joan
authors: J
authors: Villena
authors: Departamento de Química, Universidad Técnica Federico Santa María, Avenida España 1680, 2390123 Valparaíso, Chile.
authors: Patricio G
authors: PG
authors: Reveco
authors: Departamento de Química, Universidad Técnica Federico Santa María, Avenida España 1680, 2390123 Valparaíso, Chile.
authors: Franz A
authors: FA
authors: Thomet