Journal Article

DESY-2014-01384

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII

Dudutienė, V. (Corresponding author) ; Zubrienė, A. ; Smirnov, A.Extern* ; Gylytė, J. ; Timm, D. ; Manakova, E.Extern* ; Gražulis, S.Extern* ; Matulis, D.

2013
Elsevier Amsterdam [u.a.]

This record in other databases:        

Please use a persistent id in citations: doi:10.1016/j.bmc.2013.01.008

Abstract: A series of 4-substituted-2,3,5,6-tetrafluorobenezenesulfonamides were synthesized and their binding potencies as inhibitors of recombinant human carbonic anhydrase isozymes I, II, VII, XII, and XIII were determined by the thermal shift assay, isothermal titration calorimetry, and stop-flow CO2 hydration assay. All fluorinated benzenesulfonamides exhibited nanomolar binding potency toward tested CAs and fluorinated benzenesulfonamides posessed higher binding potency than non-fluorinated compounds. The crystal structures of 4-[(4,6-dimethylpyrimidin-2-yl)thio]-2,3,5,6-tetrafluorobenzenesulfonamide in complex with CA II and CA XII, and 2,3,5,6-tetrafluoro-4-[(2-hydroxyethyl)sulfonyl]benzenesulfonamide in complex with CA XIII were determined. The observed dissociation constants for several fluorinated compounds reached subnanomolar range for CA I isozyme. The affinity and the selectivity of the compounds towards tested isozymes are presented.

Note: © Elsevier Ltd. ; Post referee fulltext in progress; Embargo 12 months from publication

---

Contributing Institute(s):

1. EMBL-User (EMBL-User)

Research Program(s):

1. DORIS Beamline K1.1 (POF2-54G13) (POF2-54G13)
2. DORIS Beamline K1.3 (POF2-54G13) (POF2-54G13)

Experiment(s):

1. DORIS Beamline K1.1 (DORIS III)
2. DORIS Beamline K1.3 (DORIS III)

Appears in the scientific report 2013

---

Database coverage:
; BIOSIS Previews ; Current Contents - Life Sciences ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

---