title: Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity.
abstract: A small library of coumarins, carrying butynyl-amino chains, was synthesized continuing our studies in the field of MDR reverting ageEnts and in order to obtain multipotent agents to combat malignancies. In particular, the reported anticancer and chemopreventive natural product 7-isopentenyloxycoumarin was linked to different terminal amines, selected on the basis of our previously reported results. The anticancer behaviour and the MDR reverting ability of the new compounds were evaluated on human colon cancer cells, particularly prone to develop the MDR phenotype. Some of the new derivatives showed promising effects, directly acting as cytotoxic compounds and/or counteracting MDR phenomenon. Compound 1e emerged as the most interesting of this series, showing a multipotent biological profile and suggesting that conjugation of an appropriate coumarin core with a properly selected butynyl-amino chain allows to obtain novel hybrid molecules endowed with improved in vitro antitumor activity.
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy. Electronic address: alessandra.bisi@unibo.it.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Bisi
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy. Electronic address: concettina.cappadone@unibo.it.
authors.forename: Concettina
authors.initials: C
authors.lastname: Cappadone
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Rampa
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy; National Institute of Biostructures and Biosystems, Via delle Medaglie D'oro, 305, 00136 Roma, Italy.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Farruggia
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy.
authors.forename: Azzurra
authors.initials: A
authors.lastname: Sargenti
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Belluti
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy.
authors.forename: Rita M C
authors.initials: RMC
authors.lastname: Di Martino
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy.
authors.forename: Emil
authors.initials: E
authors.lastname: Malucelli
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy.
authors.forename: Alessia
authors.initials: A
authors.lastname: Meluzzi
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy; National Institute of Biostructures and Biosystems, Via delle Medaglie D'oro, 305, 00136 Roma, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Iotti
authors.affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Gobbi
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; C030123:coumarin
keywords: Anticancer; Chemosensitizers; Coumarin; MDR modulators; P-glycoprotein