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2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro

SYSNO ASEP	0446880
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro
Author(s)	Řezníčková, Eva (UEB-Q)_{RID, ORCID} Popa, Alexandr (UEB-Q) Gucký, Tomáš (UEB-Q)_ORCID Zatloukal, Marek (UEB-Q)_ORCID Havlíček, Libor (UEB-Q)_{RID, ORCID} Bazgier, Václav (UEB-Q)_{ORCID, RID} Berka, K. (CZ) Jorda, Radek (UEB-Q)_{ORCID, RID} Popa, Igor (UEB-Q) Nasereddin, A. (IL) Jaffe, Ch. L. (IL) Kryštof, Vladimír (UEB-Q)_{RID, ORCID} Strnad, Miroslav (UEB-Q)_{RID, ORCID}
Source Title	Bioorganic and Medicinal Chemistry Letters. - : Elsevier - ISSN 0960-894X Roč. 25, č. 11 (2015), s. 2298-2301
Number of pages	4 s.
Language	eng - English
Country	GB - United Kingdom
Keywords	Purine ; Cyclin-dependent kinase ; Leishmania
Subject RIV	EB - Genetics ; Molecular Biology
R&D Projects	LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
Institutional support	UEB-Q - RVO:61389030
UT WOS	000354115400007
DOI	10.1016/j.bmcl.2015.04.030
Annotation	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.
Workplace	Institute of Experimental Botany
Contact	David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469
Year of Publishing	2016

Number of the records: 1