Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 5, Pages 1283-1286Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.079
Keywords
Carbonic anhydrase; Isozymes; Tumor-associated enzymes; Benzenesulfonamide; Photochromism; 1,2-Dithienylethene
Categories
Funding
- European Union
- Italian FIRB [MIUR/FIRB RBNE03PX83_001]
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available