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

. 2011 Jul 15 ; 21 (14) : 4233-7. [epub] 20110527

Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/pmid21683592

Grantová podpora
G0400028 Medical Research Council - United Kingdom

Odkazy

PubMed 21683592
DOI 10.1016/j.bmcl.2011.05.076
PII: S0960-894X(11)00705-0
Knihovny.cz E-zdroje

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 1.5-12.4μM. Structure-activity relationships for the tested compounds are discussed and related to the lipophilicity of the compounds.

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. 2013 Jun 01 ; 69 (Pt 6) : o954-5. [epub] 20130525

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