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

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F11%3A33118144" target="_blank" >RIV/61989592:15310/11:33118144 - isvavai.cz</a>

Alternative codes found

RIV/61389030:_____/11:00368593

Result on the web

<a href="http://dx.doi.org/10.1016/j.bmcl.2011.05.076" target="_blank" >http://dx.doi.org/10.1016/j.bmcl.2011.05.076</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bmcl.2011.05.076" target="_blank" >10.1016/j.bmcl.2011.05.076</a>

Result language

angličtina

Original language name

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

Original language 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.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

EE - Microbiology, virology

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2011

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Bioorganic &amp; Medicinal Chemistry Letters

ISSN

0960-894X

e-ISSN

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Volume of the periodical

21

Issue of the periodical within the volume

14

Country of publishing house

GB - UNITED KINGDOM

Number of pages

5

Pages from-to

4233-4237

UT code for WoS article

000292186400024

EID of the result in the Scopus database

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