Vomasta, Daniel and Innocenti, A. and König, Burkhard and Supuran, T. (2009) Carbonic anhydrase inhibitors: Two-prong versus mono-prong inhibitors of isoformsI, II, IX and XII exemplified by photochromics cis-1,2-a-dithienylethene derivates. Bioorganic & Medicinal Chemistry Letters 19, pp. 1283-1286.
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We investigated the inhibition of five physiologically relevant CA isoforms with photochromic cis-1,2-adithienylethene-
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 (KIs 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 (KIs 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
(KIs of 1.12–16.7 lM).
|Institutions:||Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König|
|Projects:||GRK 760, Graduiertenkolleg Medizinische Chemie|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Created at the University of Regensburg:||Unknown|
|Deposited On:||05 Jun 2009 14:11|
|Last Modified:||08 Nov 2010 10:18|