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


Guzel-Akdemir O., AKDEMİR A., Karali N., Supuran C. T.

ORGANIC & BIOMOLECULAR CHEMISTRY, cilt.13, sa.23, ss.6493-6499, 2015 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 13 Sayı: 23
  • Basım Tarihi: 2015
  • Doi Numarası: 10.1039/c5ob00688k
  • Dergi Adı: ORGANIC & BIOMOLECULAR CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.6493-6499
  • İstanbul Üniversitesi Adresli: Evet

Özet

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.