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@ARTICLE{Capkauskaite:140131,
author = {Capkauskaite, E. and Zubriene, A. and Baranauskiene, L. and
Tamulaitiene, G. and Manakova, E. and Kairys, V. and
Grazulis, S. and Tumkevicius, S. and Matulis, D. and DESY},
title = {{D}esign of [(2-pyrimidinylthio)acetyl]benzenesulfonamides
as inhibitors of human carbonic anhydrases.},
journal = {European journal of medicinal chemistry},
volume = {51},
issn = {0223-5234},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {PHPPUBDB-24637},
pages = {259-70},
year = {2012},
abstract = {A series of [(2-pyrimidinylthio)acetyl]benzenesulfonamides
were designed and synthesized. Their binding affinities as
inhibitors of several recombinant human carbonic anhydrase
(CA) isozymes were determined by isothermal titration
calorimetry (ITC) and thermal shift assay (TSA). A group of
compounds containing a chlorine atom in the
benzenesulfonamide ring were found to exhibit higher
selectivity but lower binding affinity toward tested CAs.
The crystal structures of selected compounds in complex with
CA II were determined to atomic resolution. Docking studies
were performed to compare the binding modes of
experimentally determined crystallographic structures with
computational prediction of the pyrimidine derivative
binding to CA II. Several compounds bound to select CAs with
single-digit nanomolar affinities and could be used as leads
for inhibitor development toward a select CA isozyme.},
keywords = {Carbonic Anhydrase Inhibitors: chemical synthesis /
Carbonic Anhydrase Inhibitors: chemistry / Carbonic
Anhydrase Inhibitors: pharmacology / Carbonic Anhydrases:
chemistry / Carbonic Anhydrases: metabolism / Catalytic
Domain / Drug Design / Humans / Models, Molecular /
Sulfonamides: chemical synthesis / Sulfonamides: chemistry /
Sulfonamides: pharmacology / Carbonic Anhydrase Inhibitors
(NLM Chemicals) / Sulfonamides (NLM Chemicals) /
benzenesulfonamide (NLM Chemicals) / Carbonic Anhydrases
(NLM Chemicals)},
cin = {EMBL},
ddc = {610},
cid = {$I:(DE-H253)EMBL_-2012_-20130307$},
pnm = {FS Beamline without reference (POF2-544)},
pid = {G:(DE-H253)POF2-No-Ref-20130405},
experiment = {EXP:(DE-H253)Unknown-BL-20150101},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:22440859},
UT = {WOS:000304291900026},
UT = {WOS:000304291900026},
doi = {10.1016/j.ejmech.2012.02.050},
url = {https://bib-pubdb1.desy.de/record/140131},
}