Vomasta, Daniel and Innocenti, Alessio and Koenig, Burkhard and Supuran, Claudiu T. (2009) Carbonic anhydrase inhibitors: Two-prong versus mono-prong inhibitors of isoforms I, II, IX, and XII exemplified by photochromic cis-1,2-alpha-dithienylethene derivatives. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19 (5). pp. 1283-1286. ISSN 0960-894X, 1464-3405
Full text not available from this repository. (Request a copy)Abstract
We investigated the inhibition of five physiologically relevant CA isoforms with photochromic cis-1,2-alpha-dithienylethene-based compounds incorporating either a benzenesulfonamide and Cu(II)-iminodiacetic acid (IDA)-, bis-benzenesulfonamide-, bis-Cu(II)-IDA-, and bis-ethyleneglycol-methyl ether moieties, in both their open- and closed-ring forms. For hCA I the best inhibitors were the mono-prong bis-sulfonamide and the bis-Cu-IDA complexes (K(I)s of 2-3 nM) in their open form. For hCA II, best inhibitors were the open and closed forms of the mono-prong bis-sulfonamide (K(I)s of 13-18 nM). hCA IX was moderately inhibited by these compounds (KIs of 9-376 nM) whereas hCA XII and XIV were less susceptible to inhibition (K(I)s of 1.12-16.7 mu M). (C) 2009 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | TRANSMEMBRANE ISOZYME-XIV; SULFONAMIDES; ACTIVATORS; COMPLEXES; BINDING; TAILS; Carbonic anhydrase; Isozymes; Tumor-associated enzymes; Benzenesulfonamide; Photochromism; 1,2-Dithienylethene |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 21 Sep 2020 09:57 |
| Last Modified: | 21 Sep 2020 09:57 |
| URI: | https://pred.uni-regensburg.de/id/eprint/29311 |
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