2. Academic Validation
  3. Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII

Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII

  • Eur J Med Chem. 2020 Aug 15;200:112300. doi: 10.1016/j.ejmech.2020.112300.
Aiga Grandāne 1,  Alessio Nocentini 2,  Ilona Domračeva 1,  Raivis Žalubovskis 3,  Claudiu T Supuran 2
Affiliations

Affiliations

  • 1 Latvian Institute of Organic Synthesis, Aizkraukles 21, 1006, Riga, Latvia.
  • 2 Università degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, Sesto Fiorentino, Florence, 50019, Italy.
  • 3 Latvian Institute of Organic Synthesis, Aizkraukles 21, 1006, Riga, Latvia; Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, 3/7 Paula Valdena Str., Riga, 1048, Latvia. Electronic address: raivis@osi.lv.
PMID: 32460112 DOI: 10.1016/j.ejmech.2020.112300
Abstract

Oxathiino[6,5-b]pyridine 2,2-dioxides are identified as a new class of isoform-selective nanomolar inhibitors of tumor associated human carbonic anhydrases (hCA) IX and XII. At the same time they do not inhibit or poorly inhibit cytosolic isoforms hCA I and II. Oxathiino[6,5-b]pyridine 2,2-dioxides exhibited good antiproliferative properties on tumor cell lines MCF-7 (Human breast adenocarcinoma), A549 (human lung (alveolar) adenocarcinoma) and HeLa (epithelioid cervix carcinoma).

Keywords

Carbonic anhydrase; Inhibitor; Tumor; oxathiino[6,5-b]pyridine 2,2-dioxide.

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