title: Synthesis, characterization, structure, molecular modeling studies and biological activity of sterically crowded Pt(II) complexes containing bis(imidazole) ligands.
abstract: The syntheses, structures and biological evaluation of a series of cisplatin-like complexes containing bis(imidazole) derivatives - the so-called Joseph ligands - are described. Their cytotoxicity is discussed in terms of their polar surface area, rate of aquation, and lipophilicity. The X-ray crystal structure of the platinum diiodido derivative of dimethyl 2-(di(1H-imidazol-2-yl)methyl)malonate) is reported and compared to those of related systems. Molecular modeling studies are focused on the hydrogen bonding properties of such systems, and their relevance to antitumor activity.
authors.affiliation: Dipartimento di Scienze dell'Ambiente e della Vita, Università del Piemonte Orientale Amedeo Avogadro, Alessandria, Italy.
authors.forename: Mauro
authors.initials: M
authors.lastname: Ravera
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Gabano
authors.forename: Manuele
authors.initials: M
authors.lastname: Sardi
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Ermondi
authors.forename: Giulia
authors.initials: G
authors.lastname: Caron
authors.forename: Michael J
authors.initials: MJ
authors.lastname: McGlinchey
authors.forename: Helge
authors.initials: H
authors.lastname: Müller-Bunz
authors.forename: Elena
authors.initials: E
authors.lastname: Monti
authors.forename: Marzia B
authors.initials: MB
authors.lastname: Gariboldi
authors.forename: Domenico
authors.initials: D
authors.lastname: Osella
mesh_terms: D000230:Adenocarcinoma / Q000378:metabolism / Q000473:pathology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D003110:Colonic Neoplasms / Q000378:metabolism / Q000473:pathology; D018360:Crystallography, X-Ray; D005260:Female; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008024:Ligands; D008297:Male; D008958:Models, Molecular; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010051:Ovarian Neoplasms / Q000378:metabolism / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D007093:Imidazoles; D008024:Ligands; D009944:Organoplatinum Compounds; C029899:imidazole; D002945:Cisplatin