title: Influence of (hydroxymethyl)pyridine and pyridine-carboxylic acids, in trans-position to the isopropylamine and amine ligands, on the cytotoxicity of platinum complexes.
abstract: trans-Pt(II) Complexes with aliphatic amines and planar amines such as (hydroxymethyl)pyridines, and pyridine-3- and pyridine-4-carboxylic acids were synthesized and screened for their potential cytotoxic activity in different cancer cell lines used at the NCI for in vitro screens, i.e., MCF7, NCIH460, and SF268. The complexes studied were designed to differ in geometrical parameters such as the position of the phenyl-group substituents and the nature of the substituents themselves for gathering information about the structure-activity relationships in the trans-complexes. The variation of the substituents turns to be crucial for their biological activity, as both pyridine-3- and pyridine-4-carboxylic acids in trans-position to both amine and isopropylamine ligands provided complexes which displayed no specificity toward any type of cell tested, while (hydroxymethyl)pyridine in trans-position to isopropylamine ligands led to complexes that were clearly more effective against the cell lines tested.
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).
authors.forename: Rosa M
authors.initials: RM
authors.lastname: Medina
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).|Present address: School of Chemistry, Bristol University.
authors.forename: Jorge
authors.initials: J
authors.lastname: Rodríguez
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).
authors.forename: Adoración G
authors.initials: AG
authors.lastname: Quiroga
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).|Present address: Experimental Therapeutic Program, Centro Nacional de Investigaciones Oncológicas.
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: Ramos-Lima
authors.affiliation: Experimental Therapeutic Program, Centro Nacional de Investigaciones Oncológicas, ES-28029 Madrid.
authors.forename: Victoria
authors.initials: V
authors.lastname: Moneo
authors.affiliation: Experimental Therapeutic Program, Centro Nacional de Investigaciones Oncológicas, ES-28029 Madrid.
authors.forename: Amancio
authors.initials: A
authors.lastname: Carnero
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).
authors.forename: Carmen
authors.initials: C
authors.lastname: Navarro-Ranninger
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).
authors.forename: María J
authors.initials: MJ
authors.lastname: Macazaga
mesh_terms: D000588:Amines / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D006801:Humans; D006860:Hydrogen Bonding; D008024:Ligands; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017671:Platinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011437:Propylamines / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D008024:Ligands; D009944:Organoplatinum Compounds; D017671:Platinum Compounds; D011437:Propylamines; D011725:Pyridines; C035263:2-propylamine