Jorda, R. et al. (2011) Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines. Bioorganic and Medicinal Chemistry Letters, 21(14), pp. 4233-4237. (doi: 10.1016/j.bmcl.2011.05.076)
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Abstract
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 EC50 in a range 1.5–12.4 μM. Structure–activity relationships for the tested compounds are discussed and related to the lipophilicity of the compounds.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Walkinshaw, Mr Malcolm |
| Authors: | Jorda, R., Sacerdoti-Sierra, N., Voller, J., Havlíček, L., Kráčalíková, K., Nowicki, M.W., Nasereddin, A., Kryštof, V., Strnad, M., Walkinshaw, M.D., and Jaffe, C. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Biodiversity, One Health & Veterinary Medicine |
| Journal Name: | Bioorganic and Medicinal Chemistry Letters |
| Publisher: | Elsevier |
| ISSN: | 0960-894X |
| ISSN (Online): | 1464-3405 |
| Published Online: | 15 July 2011 |
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