Autor: Řezníčková, E.; Popa, A.; Gucký, T.; Zatloukal, M.; Havlíček, L.; Bazgier, V.; Berka, K.; Jorda, R.; Popa, I.; Nasereddin, A. L.; Jaffe, C.; Kryštof, V.; Strnad, M.
Název práce v češtině: 2,6,9-trisubstituované puriny jako CRK3 kinasové inhibitory s antileishmaniální aktivitou in vitro.
Název práce v angličtině: 2,6,9-trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro.
Studentská publikace: ne
Klíčová slova v češtině: Leishmania, puriny trisubstituované
Klíčová slova v angličtině: Leishmania, purines trisubstituted
Abstrakt česky: Byly syntetizovány trisubstituované puriny a změřena jejich in vitro antileishmaniální aktivita.
Abstrakt anglicky: Here we describe the leishmanicidal activities of a library of 2,6,9-trisubstituted purines that were screened for interaction with Cdc2-related protein kinase 3 (CRK3) and subsequently for activity against parasitic Leishmania species. The most active compound inhibited recombinant CRK3 with an IC50 value of 162 nM and was active against Leishmania major and Leishmania donovani at low micromolar concentrations in vitro. Its mode of binding to CRK3 was investigated by molecular docking using a homology model.
Jazyk v originále: Anglický
Název časopisu: Bioorg. Med. Chem. Lett.
Rok: 2015
Svazek (ročník): 25
Číslo časopisu v rámci uvedeného svazku: 11
Strana od-do: 2298-2301

Q1: ne

ISSN časopisu: 0960-894X
Vydavatel: Elsevier
Způsob financování: Ministry of Education, Youth and Sports of the Czech Republic (LO1305, LO1204), the European Regional Development Fund and the State Budget of the Czech Republic (RECAMO, CZ.1.05/2.1.00/03.0101), the Operational Program Research and Development for Innovations (IMTM project CZ.1.05/2.1.00/01.0030), Palacký University in Olomouc (IGA_PrF_2015_027, IGA_PrF_2014_024 and IGA_PrF_2015_021) and the German Federal Ministry of Education and Research (Bio-Disc 5 project 315729).