Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors(252 views visite) La Regina G, Coluccia A, Famiglini V, Pelliccia S, Monti L, Vullo D, Nuti E, Alterio V, De Simone G, Monti SM, Pan P, Parkkila S, Supuran CT, Rossello A, Silvestri R
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2015 Nov 12; 58(21): 8564-8572.
Keywords Parole chiave: Not available. Non disponibili.
Affiliations Affiliazioni: *** IBB - CNR ***
Istituto Pasteur Italia-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma , Piazzale Aldo Moro 5, I-00185 Roma, Italy. Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Universita di Firenze , Via Ugo Schiff 6, I-50019 Sesto Fiorentino, Firenze, Italy. Dipartimento di Farmacia, Universita di Pisa , Via Bonanno Pisano 6, I-56126 Pisa, Italy. Istituto di Biostrutture e Bioimmmagini, Consiglio Nazionale delle Ricerche , Via Mezzocannone 16, I-80134 Napoli, Italy. School of Medicine, University of Tampere and Tampere University Hospital , 33014 Tampere, Finland.
References Riferimenti: Not available. Non disponibili.
Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors
New 1,1'-biphenylsulfonamides were synthesized and evaluated as inhibitors of the ubiquitous human carbonic anhydrase isoforms I, II, IX, XII, and XIV using acetazolamide (AAZ) as reference compound. The sulfonamides 1-21 inhibited all the isoforms, with Ki values in the nanomolar range of concentration, and were superior to AAZ against all of them. X-ray crystallography and molecular modeling studies on the adducts that compound 20, the most potent hCA XIV inhibitor of the series (Ki = 0.26 nM), formed with the five hCAs, provided insight into the molecular determinants responsible for the high affinity of this molecule toward the target enzymes. The results pave the way to the development of 1.1'-biphenylsulfonamides as a new class of highy potent hCA XIV inhibitors.
Discovery of 1, 1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors
Petraglia F, Singh AA, Carafa V, Nebbioso A, Conte M, Scisciola L, Valente S, Baldi A, Mandoli A, Petrizzi VB, Ingenito C, De Falco S, Cicatiello V, Apicella I, Janssen-megens EM, Kim B, Yi G, Logie C, Heath S, Ruvo M, Wierenga ATJ, Flicek P, Yaspo ML, Della Valle V, Bernard O, Tomassi S, Novellino E, Feoli A, Sbardella G, Gut I, Vellenga E, Stunnenberg HG, Mai A, Martens JHA, Altucci L * Combined HAT/EZH2 modulation leads to cancer-selective cell death(199 visite) Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2018 May 22; 9(39): 25630-25646. Impact Factor:5.008 DettagliEsporta in BibTeXEsporta in EndNote
350 Records (325 escludendo Abstract e Conferenze). Impact factor totale: 1422.351 (1339.464 escludendo Abstract e Conferenze). Impact factor a 5 anni totale: 1350.549 (1257.937 escludendo Abstract e Conferenze).
Last modified by Ultima modifica di Vincenzo Alterio on in data Sunday 12 July 2020, 13:14:48 252 views visite. Last view on Ultima visita in data Saturday 23 January 2021, 2:38:10