Discovery of novel isatin-based sulfonamides with potent and selective inhibition of the tumor-associated carbonic anhydrase isoforms IX and XII

Özlen Güzel-Akdemir; Atilla Akdemir; Nilgün Karalı; Claudiu T. Supuran

doi:10.1039/C5OB00688K

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Discovery of novel isatin-based sulfonamides with potent and selective inhibition of the tumor-associated carbonic anhydrase isoforms IX and XII

Özlen Güzel-Akdemir, Atilla Akdemir, Nilgün Karalı and Claudiu T. Supuran
Org. Biomol. Chem., 2015,13, 6493-6499
DOI: 10.1039/C5OB00688K, Paper

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Abstract | Cited by

A series of 2/3/4-[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]benzenesulfonamides, obtained from substituted isatins and 2-, 3- or 4-aminobenzenesulfonamide, showed low nanomolar inhibitory activity against the tumor associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX and XII – recently validated antitumor drug targets, being much less effective as inhibitors of the off-target cytosolic isoforms CA I and II.

Graphical abstract: Discovery of novel isatin-based sulfonamides with potent and selective inhibition of the tumor-associated carbonic anhydrase isoforms IX and XII

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