13420-80-9Relevant articles and documents
Synthesis and preliminary evaluation in tumor bearing mice of new 18F-labeled arylsulfone matrix metalloproteinase inhibitors as tracers for positron emission tomography
Casalini, Francesca,Fugazza, Lorenza,Esposito, Giovanna,Cabella, Claudia,Brioschi, Chiara,Cordaro, Alessia,D'Angeli, Luca,Bartoli, Antonietta,Filannino, Azzurra M.,Gringeri, Concetta V.,Longo, Dario L.,Muzio, Valeria,Nuti, Elisa,Orlandini, Elisabetta,Figlia, Gianluca,Quattrini, Angelo,Tei, Lorenzo,Digilio, Giuseppe,Rossello, Armando,Maiocchi, Alessandro
, p. 2676 - 2689 (2013/05/22)
New fluorinated, arylsulfone-based matrix metalloproteinase (MMP) inhibitors containing carboxylate as the zinc binding group were synthesized as radiotracers for positron emission tomography. Inhibitors were characterized by Ki for MMP-2 in th
Exploring the neuroleptic substituent in octoclothepin: Potential ligands for positron emission tomography with subnanomolar affinity for α1-adrenoceptors
Kristensen, Jesper L.,Püschl, Ask,Jensen, Martin,Risgaard, Rune,Christoffersen, Claus T.,Bang-Andersen, Benny,Balle, Thomas
experimental part, p. 7021 - 7034 (2010/11/18)
A series of 1-(10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine analogues substituted in the 8-position of the 10,11-dihydrodibenzo[b,f]thiepine scaffold with aryl, heteroaryl, amine, and amide substituents are described. The compounds were designed using the previously reported Liljefors- B?ges? pharmacophore model for dopamine D2 and α1-adrenoceptor antagonists, with the aim of obtaining selective α1-adrenoceptor antagonists suitable for development as radioligands for imaging of central α1-adrenoceptors by positron emission tomography. Sixteen aryl and heteroaryl substituted octoclothepin analogues were prepared by a convergent synthesis via coupling of 1-methyl-4-(8-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-10, 11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine with aryl and heteroaryl halides under palladium catalysis. The most selective compound obtained, (S)-N-((11-(4-methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl) methyl)isobutyramide (S)-35, showed a similar subnanomolar affinity compared to α1a, α1b, and α1d- adrenoceptors and a selectivity ratio of 20, 440, and 20 with respect to D 2, 5-HT2C, and H1 receptors, respectively.
THIOARYL SUBSTITUTED INHIBITORS OF ZINC PROTEASES AND THEIR USE
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Page/Page column 40-41, (2009/10/01)
There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibi
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors
Nuti, Elisa,Panelli, Laura,Casalini, Francesca,Avramova, Stanislava I.,Orlandini, Elisabetta,Santamaria, Salvatore,Nencetti, Susanna,Tuccinardi, Tiziano,Martinelli, Adriano,Cercignani, Giovanni,D'Amelio, Nicola,Maiocchi, Alessandro,Uggeri, Fulvio,Rossello, Armando
experimental part, p. 6347 - 6361 (2010/03/24)
Overexpression of macrophage elastase (MMP-12), a member of the matrix metalloproteinases family, can be linked to tissue remodeling and degradation in some inflammatory processes, such as chronic obstructive pulmonary disease (COPD), emphysema, rheumatoi
INHIBITORS OF ZINC PROTEASES THIOARYL SUBSTITUTED AND THEIR USE
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Page/Page column 59-60; 86-87, (2008/06/13)
There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibi