Počet záznamů: 1
Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines
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SYSNO ASEP 0368593 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines Tvůrce(i) Jorda, Radek (UEB-Q) ORCID, RID
Sacerdoti-Sierra, N. (IL)
Voller, Jiří (UEB-Q) RID, ORCID
Havlíček, Libor (UEB-Q) RID, ORCID
Kráčalíková, Kateřina (UEB-Q)
Nowicki, M. W. (GB)
Nasereddin, A. (IL)
Kryštof, Vladimír (UEB-Q) RID, ORCID
Strnad, Miroslav (UEB-Q) RID, ORCID
Walkinshaw, M. D. (GB)
Jaffe, Ch. L. (IL)Celkový počet autorů 11 Zdroj.dok. Bioorganic and Medicinal Chemistry Letters. - : Elsevier - ISSN 0960-894X
Roč. 21, č. 14 (2011), s. 4233-4237Poč.str. 5 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova Leishmania ; Cyclin-dependent kinase ; Inhibitor ; Therapy Vědní obor RIV EE - Mikrobiologie, virologie CEP GA204/08/0511 GA ČR - Grantová agentura ČR GA301/08/1649 GA ČR - Grantová agentura ČR CEZ AV0Z50380511 - UEB-Q (2005-2011) UT WOS 000292186400024 DOI 10.1016/j.bmcl.2011.05.076 Anotace 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. Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2012
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