期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 11, 页码 2298-2301出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.04.030
关键词
Purine; Inhibitor; Cyclin-dependent kinase; Leishmania
资金
- Ministry of Education, Youth and Sports of the Czech Republic [LO1305, LO1204]
- European Regional Development Fund
- State Budget of the Czech Republic (RECAMO) [CZ.1.05/2.1.00/03.0101]
- Operational Program Research and Development for Innovations (IMTM project) [CZ.1.05/2.1.00/01.0030]
- Palacky University in Olomouc [IGA_PrF_2015_027, IGA_PrF_2014_024, IGA_PrF_2015_021]
- German Federal Ministry of Education and Research [315729]
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. (C) 2015 Elsevier Ltd. All rights reserved.
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