title: In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety.
abstract: The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9µM) and more effective than cisplatin on both DLD-1 (IC50=57.4µM) and MCF-7 (IC50=79.9µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmaceutiche, Via Venezian 21, 20133 Milan, Italy. Electronic address: isabella.rimoldi@unimi.it.
authors.forename: Isabella
authors.initials: I
authors.lastname: Rimoldi
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmaceutiche, Via Venezian 21, 20133 Milan, Italy.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Facchetti
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Agrarie e Ambientali-Produzione, Territorio, Agroenergia, Via Celoria 2, 20133 Milan, Italy.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Lucchini
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmacologiche e Biomolecolari; Via Balzaretti 9, 20133 Milan, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Castiglioni
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmacologiche e Biomolecolari; Via Balzaretti 9, 20133 Milan, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Marchianò
authors.affiliation: Università degli Studi di Padova, Dipartimento di Scienze del Farmaco, Via Marzolo 5, 35131 Padua, Italy.
authors.forename: Nicola
authors.initials: N
authors.lastname: Ferri
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D056148:Chromatography, Reverse-Phase; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000494:pharmacology*; D064726:Triple Negative Breast Neoplasms / Q000473:pathology*
chemical_list: D000970:Antineoplastic Agents; D007093:Imidazoles; D009944:Organoplatinum Compounds
keywords: Cationic platinum complex; Cell cycle; Imidazole; Triple negative breast cancer; p53 expression