4-[N-(Substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII

被引：31

作者：

Sudzius, Jurgis ^{[2
]}

Baranauskiene, Lina ^{[1
]}

Golovenko, Dmitrij ^{[3
]}

Matuliene, Jurgita ^{[1
]}

Michailoviene, Vilma ^{[1
]}

Torresan, Jolanta ^{[1
]}

Jachno, Jelena ^{[1
]}

Sukackaite, Rasa ^{[3
]}

Manakova, Elena ^{[3
]}

Grazulis, Saulius ^{[3
]}

Tumkevicius, Sigitas ^{[2
]}

Matulis, Daumantas ^{[1
]}

机构：

[1] Inst Biotechnol, Lab Biothermodynam & Drug Design, LT-02241 Vilnius, Lithuania

[2] Vilnius Univ, Fac Chem, Dept Organ Chem, LT-03225 Vilnius, Lithuania

[3] Inst Biotechnol, Lab Protein DNA Interact, LT-02241 Vilnius, Lithuania

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 21期

关键词：

Carbonic anhydrase isozymes I; II; VII; and XIII; Isothermal titration calorimetry; Thermal shift assay; ThermoFluor (R); Benzenesulfonamide; Pyrimidine; MODEL; MOLSCRIPT; PROTEINS; DESIGN; POTENT;

D O I：

10.1016/j.bmc.2010.09.011

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 4-[N-(substituted 4-pyrimidinyl)amino] benzenesulfonamides were designed and synthesised. Their binding potencies as inhibitors of selected recombinant human carbonic anhydrase (hCA) isozymes I, II, VII, and XIII were measured using isothermal titration calorimetry and the thermal shift assay. To determine the structural features of inhibitor binding, the crystal structures of several compounds in complex with hCA II were determined. Several compounds exhibited selectivity towards isozymes I, II, and XIII, and some were potent inhibitors of hCA VII. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7413 / 7421

页数：9

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