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9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XII.
Göksu, Haydar; Topal, Meryem; Keskin, Ali; Gültekin, Mehmet S; Çelik, Murat; Gülçin, Ilhami; Tanc, Muhammet; Supuran, Claudiu T.
Affiliation
  • Göksu H; Kaynasli Vocational College, Düzce University, Düzce, Turkey.
  • Topal M; Faculty of Science, Department of Chemistry, Atatürk University, Erzurum, Turkey.
  • Keskin A; Department of Medical Services and Techniques, Vocational School of Health Services, Gumushane University, Gumushane, Turkey.
  • Gültekin MS; Faculty of Science, Department of Chemistry, Atatürk University, Erzurum, Turkey.
  • Çelik M; Faculty of Science, Department of Chemistry, Atatürk University, Erzurum, Turkey.
  • Gülçin I; Faculty of Science, Department of Chemistry, Atatürk University, Erzurum, Turkey.
  • Tanc M; Faculty of Science, Department of Chemistry, Atatürk University, Erzurum, Turkey.
  • Supuran CT; Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
Arch Pharm (Weinheim) ; 349(6): 466-74, 2016 Jun.
Article in En | MEDLINE | ID: mdl-27174792
N-substituted maleimides were synthesized from maleic anhydride and primary amines. 1,4-Dibromo-dibenzo[e,h]bicyclo-[2,2,2]octane-2,3-dicarboximide derivatives (4a-f) were prepared by the [4+2] cycloaddition reaction of dibromoanthracenes with the N-substituted maleimide derivatives. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new derivatives were assayed against the human (h) isozymes hCA I, II, IX, and XII. All tested bicyclo dicarboximide derivatives exhibited excellent inhibitory effects in the nanomolar range, with Ki values in the range of 117.73-232.87 nM against hCA I and of 69.74-111.51 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and XII.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Carbonic Anhydrase Inhibitors / Carbonic Anhydrases / Anthracenes Limits: Humans Language: En Journal: Arch Pharm (Weinheim) Year: 2016 Document type: Article Affiliation country: Country of publication:

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Carbonic Anhydrase Inhibitors / Carbonic Anhydrases / Anthracenes Limits: Humans Language: En Journal: Arch Pharm (Weinheim) Year: 2016 Document type: Article Affiliation country: Country of publication: