Počet záznamů: 1

Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as Potent Carbonic AnhydraseInhibitors: Synthesis, Biological Evaluation, and Enzyme-Ligand X-ray Studies

  1. 1.
    0343450 - UOCHB-X 2011 RIV US eng J - Článek v odborném periodiku
    Gitto, R. - Agnello, S. - Ferro, S. - De Luca, L. - Vullo, D. - Brynda, Jiří - Mader, Pavel - Supuran, C. T. - Chimirri, A.
    Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as Potent Carbonic AnhydraseInhibitors: Synthesis, Biological Evaluation, and Enzyme-Ligand X-ray Studies.
    Journal of Medicinal Chemistry. Roč. 53, č. 6 (2010), s. 2401-2408 ISSN 0022-2623
    Grant CEP: GA ČR GA203/09/0820
    Výzkumný záměr: CEZ:AV0Z40550506; CEZ:AV0Z50520514
    Klíčová slova: inhibitor design * crystal structure * X-ray analysis * dehalogenase
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 5.207, rok: 2010

    This work explores inhibitory effects a small class of 1-(cyclo)alkylisoquinolines containing a sulfonamide function on the activity of carbonic anhydrase (CA, EC 4.2.1.1). Some derivatives showed potent hCA IX and hCA XIV inhibitory effects at nanomolar concentrations as well as low affinity for the ubiquitous hCA II. We also report the X-ray crystal structure of one of these derivatives in complex with dominant human isoform II.
    Trvalý link: http://hdl.handle.net/11104/0185928