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Thiazole-substituted benzenesulfonamides as inhibitors of 12 human carbonic anhydrases.

Abstract：

:Four series of para or meta - substituted thiazolylbenzenesulfonamides bearing Cl substituents were designed, synthesized, and evaluated as inhibitors of all 12 catalytically active recombinant human carbonic anhydrase (CA) isoforms. Observed affinities were determined by the fluorescent thermal shift assay and the intrinsic affinities were calculated based on the fractions of binding-ready deprotonated sulfonamide and CA bearing protonated hydroxide bound to the catalytic Zn(II) in the active site. Several compounds exhibited selectivity towards CA IX, an anticancer target. Intrinsic affinities reached 30 pM, while the observed affinities - 70 nM. The structure-intrinsic affinity relationship map of the compounds showed the energetic contributions of the thiazole ring and its substituents.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Čapkauskaitė E,Zubrienė A,Paketurytė V,Timm DD,Tumkevičius S,Matulis D

doi

10.1016/j.bioorg.2018.02.004

subject

Has Abstract

pub_date

2018-04-01 00:00:00

pages

534-541

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(17)30913-6

journal_volume

77

pub_type

杂志文章

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