% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@ARTICLE{apkauskait:166504,
author = {Čapkauskaitė, Edita and Zubrienė, Asta and Smirnov,
Alexey and Torresan, Jolanta and Kišonaitė, Miglė and
Kazokaitė, Justina and Gylytė, Joana and Michailovienė,
Vilma and Jogaitė, Vaida and Manakova, Elena and Gražulis,
Saulius and Tumkevičius, Sigitas and Matulis, Daumantas},
title = {{B}enzenesulfonamides with pyrimidine moiety as inhibitors
of human carbonic anhydrases {I}, {II}, {VI}, {VII}, {XII},
and {XIII}},
journal = {Bioorganic $\&$ medicinal chemistry},
volume = {21},
number = {22},
issn = {0968-0896},
address = {Amsterdam [u.a.]},
publisher = {Elsevier},
reportid = {DESY-2014-01386},
pages = {6937 - 6947},
year = {2013},
note = {© Elsevier Ltd. ; Post referee fulltext in progress;
Embargo 12 months from publication},
abstract = {Two groups of benzenesulfonamide derivatives, bearing
pyrimidine moieties, were designed and synthesized as
inhibitors of carbonic anhydrases (CA). Their binding
affinities to six recombinant human CA isoforms I, II, VI,
VII, XII, and XIII were determined by the thermal shift
assay (TSA). The binding of several inhibitors was measured
by isothermal titration calorimetry (ITC). Direct
demonstration of compound inhibition was achieved by
determining the inhibition constant by stopped-flow CO2
hydration assay. The most potent compounds demonstrated
selectivity towards isoform I and affinities of 0.5nM. The
crystal structures of selected compounds in complex with CA
II, XII, and XIII were determined to atomic resolution.
Compounds described here were compared with previously
published pyrimidinebenzenesulfonamides.(1) Systematic
structure-activity analysis of 40 compound interactions with
six isoforms yields clues for the design of compounds with
greater affinities and selectivities towards target CA
isoforms.},
cin = {EMBL-User},
ddc = {540},
cid = {I:(DE-H253)EMBL-User-20120814},
pnm = {PETRA Beamline P14 (POF2-54G14) / DORIS Beamline K1.1
(POF2-54G13)},
pid = {G:(DE-H253)POF2-P14-20130405 /
G:(DE-H253)POF2-K1.1-20130405},
experiment = {EXP:(DE-H253)P-P14-20150101 / EXP:(DE-H253)D-K1.1-20150101},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000325759800009},
pubmed = {pmid:24103428},
doi = {10.1016/j.bmc.2013.09.029},
url = {https://bib-pubdb1.desy.de/record/166504},
}