Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases

Karali N., AKDEMİR A., Goktas F., Elma P. E., Angeli A., Kizilirmak M., ...Daha Fazla

BIOORGANIC & MEDICINAL CHEMISTRY, cilt.25, sa.14, ss.3714-3718, 2017 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 25 Sayı: 14
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1016/j.bmc.2017.05.029
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.3714-3718
  • Anahtar Kelimeler: Carbonic anhydrase, Isatin, 2-Indolinone, Docking, IN-VITRO ANTICANCER, ISATIN-BETA-THIOSEMICARBAZONES, MULTIDRUG-RESISTANT CELLS, ANTITUBERCULOSIS ACTIVITY, DERIVATIVES, ANALOGS, AGENTS, CYTOTOXICITY, COMPLEXES, LIGANDS
  • İstanbul Üniversitesi Adresli: Evet

Özet

Human carbonic anhydrases IX and XII are upregulated in many tumors and form a novel target for new generation anticancer drugs. Here we report the synthesis of novel 2-indolinone derivatives with the sulfonamide group as a zinc binding moiety. Enzyme inhibition assays confirmed that the compounds showed selectivity against hCA IX and XII over the widely distributed off-targets hCA I and II. Molecular modelling studies were performed to suggest modes of binding for these compounds. (C) 2017 Elsevier Ltd. All rights reserved.