Zinātniskās darbības atbalsta sistēma
Latviešu English

Publikācija: 3H-1

Publikācijas veids Zinātniskais raksts, kas indeksēts Web of science un/vai Scopus datu bāzē
Pamatdarbībai piesaistītais finansējums Nav zināms
Aizstāvēšana: ,
Publikācijas valoda English (en)
Nosaukums oriģinālvalodā 3H-1,2-Benzoxathiepine 2,2-Dioxides: a New Class of Isoform-Selective Carbonic Anhydrase Inhibitors
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Aleksandrs Pustenko
Dmitrijs Stepanovs
Raivis Žalubovskis
Daniela Vullo
Andris Kazaks
Janis Leitans
Kaspars Tārs
Claudiu Supuran
Atslēgas vārdi Carbonic anhydrase, sulfocoumarin, homo-sulfocoumarins, inhibitor
Anotācija A new chemotype with carbonic anhydrase (CA, EC 4.2.1.1) inhibitory action has been discovered, the homo-sulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) which have been designed considering the (sulfo)coumarins as lead molecules. An original synthetic strategy of a panel of such derivatives led to compounds with a unique inhibitory profile and very high selectivity for the inhibition of the tumour associated (CA IX/XII) over the cytosolic (CA I/II) isoforms. Although the CA inhibition mechanism with these new compounds is unknown for the moment, we hypothesize that it may be similar to that of the sulfocoumarins, i.e. hydrolysis to the corresponding sulfonic acids which thereafter anchor to the zinc-coordinated water molecule within the enzyme active site.
DOI: 10.1080/14756366.2017.1316720
Hipersaite: http://www.tandfonline.com/doi/full/10.1080/14756366.2017.1316720 
Atsauce Pustenko, A., Stepanovs, D., Žalubovskis, R., Vullo, D., Kazaks, A., Leitans, J., Tārs, K., Supuran, C. 3H-1,2-Benzoxathiepine 2,2-Dioxides: a New Class of Isoform-Selective Carbonic Anhydrase Inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, 2017, Vol.32, Iss.1, 767.-775.lpp. ISSN 1475-6366. e-ISSN 1475-6374. Pieejams: doi:10.1080/14756366.2017.1316720
Papildinformācija Citējamību skaits:
ID 25566