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Publikācija: Aryl Derivatives of 3H-1

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā Aryl Derivatives of 3H-1,2-benzoxathiepine 2,2-Dioxide as Carbonic Anhydrase Inhibitors
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Pētniecības platforma Materiāli, procesi un tehnoloģijas
Autori Aleksandrs Pustenko
A. Nocentini
A. Alafeefy
A. Balašova
M. Krasavin
Raivis Žalubovskis
C.T. Supuran
Atslēgas vārdi Carbonic anhydrase, homosulfocoumarin, isoform-selective inhibitor, sulfocoumarin, transmembrane, soforms
Anotācija A new series of homosulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) possessing various substitution patterns and moieties in the 7, 8 or 9 position of the heterocylic ring were prepared by original procedures and investigated for the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the human (h) hCA I, II, IX and XII. The 8-substituted homosulfocoumarins were the most effective hCA IX/XII inhibitors followed by the 7-substituted derivatives, whereas the substitution pattern in position 9 led to less effective binders for the transmembrane, tumour-associated isoforms IX/XII. The cytosolic isoforms hCA I and II were not inhibited by these compounds, similar to the sulfocoumarins/coumarins investigated earlier. As hCA IX and XII are validated anti-tumour targets, with one sulphonamide (SLC-0111) in Phase Ib/II clinical trials, finding derivatives with better selectivity for inhibiting the tumour-associated isoforms over the cytosolic ones, as the homosulfocoumarins reported here, is of crucial importance.
DOI: 10.1080/14756366.2019.1695795
Hipersaite: https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1695795 
Atsauce Pustenko, A., Nocentini, A., Alafeefy, A., Balašova, A., Krasavin, M., Žalubovskis, R., Supuran, C. Aryl Derivatives of 3H-1,2-benzoxathiepine 2,2-Dioxide as Carbonic Anhydrase Inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, 2020, Vol. 35, No. 1, 245.-254.lpp. ISSN 1475-6366. e-ISSN 1475-6374. Pieejams: doi:10.1080/14756366.2019.1695795
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