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rdf:type
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Description
| - We report here results of screening directed to finding new anti-leishmanial drugs among 2,6-disubstituted purines and corresponding 3,7-disubstituted pyrazolo[4,3-d]pyrimidines. These compounds have previously been shown to moderately inhibit human cyclin-dependent kinases. Since some compounds reduced viability of axenic amastigotes of Leishmania donovani, we screened them for interaction with recombinant leishmanial cdc-2 related protein kinase (CRK3/CYC6), an important cell cycle regulator of the parasitic protozoan. Eighteen pairs of corresponding isomers were tested for viability of amastigotes and for inhibition of CRK3/CYC6 kinase activity. Some compounds (9A, 12A and 13A) show activity against amastigotes with EC(50) in a range 1.5-12.4 mu M. Structure-activity relationships for the tested compounds are discussed and related to the lipophilicity of the compounds. (C) 2011 Elsevier Ltd. All rights reserved.
- We report here results of screening directed to finding new anti-leishmanial drugs among 2,6-disubstituted purines and corresponding 3,7-disubstituted pyrazolo[4,3-d]pyrimidines. These compounds have previously been shown to moderately inhibit human cyclin-dependent kinases. Since some compounds reduced viability of axenic amastigotes of Leishmania donovani, we screened them for interaction with recombinant leishmanial cdc-2 related protein kinase (CRK3/CYC6), an important cell cycle regulator of the parasitic protozoan. Eighteen pairs of corresponding isomers were tested for viability of amastigotes and for inhibition of CRK3/CYC6 kinase activity. Some compounds (9A, 12A and 13A) show activity against amastigotes with EC(50) in a range 1.5-12.4 mu M. Structure-activity relationships for the tested compounds are discussed and related to the lipophilicity of the compounds. (C) 2011 Elsevier Ltd. All rights reserved. (en)
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Title
| - Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines
- Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines (en)
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skos:prefLabel
| - Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines
- Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines (en)
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skos:notation
| - RIV/61389030:_____/11:00368593!RIV12-AV0-61389030
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
| - P(GA204/08/0511), P(GA301/08/1649), Z(AV0Z50380511), Z(MSM6198959216)
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/61389030:_____/11:00368593
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - Leishmania; Cyclin-dependent kinase; Inhibitor; Therapy (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Bioorganic and Medicinal Chemistry Letters
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Havlíček, Libor
- Jaffe, Ch. L.
- Jorda, Radek
- Kryštof, Vladimír
- Kráčalíková, Kateřina
- Nasereddin, A.
- Nowicki, M. W.
- Sacerdoti-Sierra, N.
- Strnad, Miroslav
- Voller, Jiří
- Walkinshaw, M. D.
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http://linked.open...ain/vavai/riv/wos
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http://linked.open...n/vavai/riv/zamer
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issn
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number of pages
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http://bibframe.org/vocab/doi
| - 10.1016/j.bmcl.2011.05.076
|