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

被引:58
作者
Guzel-Akdemir, Ozlen [1 ]
Akdemir, Atilla [2 ]
Karali, Nilgun [1 ]
Supuran, Claudiu T. [3 ]
机构
[1] Istanbul Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34116 Istanbul, Turkey
[2] Bezmialem Vakif Univ, Fac Pharm, Dept Pharmacol, TR-34093 Istanbul, Turkey
[3] Univ Florence, NEUROFARBA Dept, Sez Sci Farmaceut, I-50019 Florence, Italy
关键词
ZINC-COMPLEXES; DRUG DESIGN; SCHIFF-BASES; PATENT; ALPHA; DERIVATIVES; CLONING; ANTIBACTERIAL; EXPRESSION; ACTIVATORS;
D O I
10.1039/c5ob00688k
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:6493 / 6499
页数:7
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