Publication: Novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors.
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Date
2018-12-01
Authors
Authors
DEMIR, K
Akdemir, ATİLLA
ANGELI, A
GÜZEL-AKDEMIR, Ö
SUPURAN, CT
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Abstract
A small collection of 26 structurally novel thiazolidinone-containing compounds, without the well-known
sulphonamide zinc-binding group, were synthesised and tested in enzyme inhibition assays against the
tumour-associated hCA IX enzyme. Inhibition constants in the lower micromolar region (KI < 25 lM) have
been measured for 17 of the 26 compounds. Even though the KI values are relatively weak, the fact that
they do not contain a sulphonamide moiety suggests that these compounds do not interact with the
active site zinc ion. Therefore, docking studies and molecular dynamics simulations have been performed
to suggest binding poses for these structurally novel inhibitors.
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Citation
GÜZEL-AKDEMIR Ö., ANGELI A., DEMIR K., SUPURAN C., Akdemir A., -Novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors.-, Journal of enzyme inhibition and medicinal chemistry, cilt.33, ss.1299-1308, 2018