title: Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors.
abstract: The most frequently used treatment for hormone receptor positive breast cancer in post-menopausal women are aromatase inhibitors. In order to develop new aromatase inhibitors, we designed and synthesized new imidazolylmethylpiperidine sulfonamides using the structure of the previously identified aromatase inhibitor SYN 20028567 as starting lead. By this approach, three new aromatase inhibitors with IC50 values that are similar to that of letrozole and SYN 20028567 were identified.
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Mauro
authors.initials: M
authors.lastname: Di Matteo
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Ammazzalorso
authors.affiliation: Department of Experimental, Diagnostic and Specialty Medicine (DIMES), Alma Mater Studiorum, University of Bologna, Via S. Giacomo 14, 40126 Bologna, Italy.
authors.forename: Federico
authors.initials: F
authors.lastname: Andreoli
authors.affiliation: Department of Internal Medicine, University of Genoa, V.le Benedetto XV 6, 16132 Genoa, Italy; IRCCS AOU San Martino-IST, Istituto Nazionale per la Ricerca sul Cancro, Genoa, Italy.
authors.forename: Irene
authors.initials: I
authors.lastname: Caffa
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: De Filippis
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Marialuigia
authors.initials: M
authors.lastname: Fantacuzzi
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Letizia
authors.initials: L
authors.lastname: Giampietro
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Cristina
authors.initials: C
authors.lastname: Maccallini
authors.affiliation: Department of Internal Medicine, University of Genoa, V.le Benedetto XV 6, 16132 Genoa, Italy; IRCCS AOU San Martino-IST, Istituto Nazionale per la Ricerca sul Cancro, Genoa, Italy.
authors.forename: Alessio
authors.initials: A
authors.lastname: Nencioni
authors.affiliation: Institute of Organic Synthesis and Photoreactivity (ISOF), National Research Council (CNR), Via P. Gobetti 101, 40129 Bologna, Italy.
authors.forename: Marco Daniele
authors.initials: MD
authors.lastname: Parenti
authors.affiliation: Department of Internal Medicine, University of Genoa, V.le Benedetto XV 6, 16132 Genoa, Italy; IRCCS AOU San Martino-IST, Istituto Nazionale per la Ricerca sul Cancro, Genoa, Italy.
authors.forename: Debora
authors.initials: D
authors.lastname: Soncini
authors.affiliation: Institute of Organic Synthesis and Photoreactivity (ISOF), National Research Council (CNR), Via P. Gobetti 101, 40129 Bologna, Italy; Innovamol Srls, Viale Alfeo Corrassori 24, Modena 41124, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Del Rio
authors.affiliation: Department of Pharmacy, University of Chieti 'G. d'Annunzio', via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Rosa
authors.initials: R
authors.lastname: Amoroso
mesh_terms: D001141:Aromatase / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047072:Aromatase Inhibitors; D010880:Piperidines; D013449:Sulfonamides; D001141:Aromatase
keywords: Anticancer agents; Aromatase inhibitor; Imidazole; Sulfonamide; Synthesis