About: Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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)
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)
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)
skos:notation	RIV/61389030:_____/11:00368593!RIV12-AV0-61389030
http://linked.open...avai/predkladatel	Ústav experimentální botaniky AV ČR, v.v.i.
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(GA204/08/0511), P(GA301/08/1649), Z(AV0Z50380511), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	14
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Kráčalíková, Kateřina Jorda, Radek Voller, Jiří Havlíček, Libor Kryštof, Vladimír Strnad, Miroslav
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	186457
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/11:00368593
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Leishmania; Cyclin-dependent kinase; Inhibitor; Therapy (en)
http://linked.open.../riv/klicoveSlovo	Cyclin-dependent kinase Inhibitor Leishmania Therapy
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[E33D541EF911]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	EE
http://linked.open...ichTvurcuVysledku	6 (xsd:int)
http://linked.open...cetTvurcuVysledku	11 (xsd:int)
http://linked.open...vavai/riv/projekt	Biological activity of synthetic inhibitors of cyclin-dependent kinases Modulation of cell division of normal and cancer cells by cyclin-dependent kinase inhibitors
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	21
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.
http://linked.open...ain/vavai/riv/wos	000292186400024
http://linked.open...n/vavai/riv/zamer	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0960-894X
number of pages	5 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2011.05.076
is http://linked.open...avai/riv/vysledek of	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

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