dc.contributor.author | Lourens, Anna C.U. | |
dc.contributor.author | Gravestock, David | |
dc.contributor.author | Van Zyl, Robyn L. | |
dc.contributor.author | Hoppe, Heinrich C. | |
dc.contributor.author | Kolesnikova, Natasha | |
dc.date.accessioned | 2017-05-12T11:10:20Z | |
dc.date.available | 2017-05-12T11:10:20Z | |
dc.date.issued | 2016 | |
dc.identifier.citation | Lourens, A.C.U. et al. 2016. Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates . Organic and biomolecular chemistry, 14(33):7899-7911. [https://doi.org/10.1039/C6OB01350C] | en_US |
dc.identifier.issn | 1477-0520 | |
dc.identifier.issn | 1477-0539 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/21939 | |
dc.identifier.uri | http://pubs.rsc.org/en/Content/ArticleLanding/2016/OB/C6OB01350C#!divAbstract | |
dc.identifier.uri | https://doi.org/10.1039/C6OB01350C | |
dc.description.abstract | The design, synthesis and biological evaluation of a series of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-
diamines is described. These compounds exhibited in vitro antiplasmodial activity in the low nanomolar range
against both drug sensitive and drug resistant strains of P. falciparum, with 1-(3-(2,4-dichlorophenoxy)
propyl)-6-phenyl-1,6-dihydro-1,3,5-triazine-2,4-diamine hydrochloride identified as the most potent
compound from this series against the drug resistant FCR-3 strain (IC50 2.66 nM). The compounds were
not toxic to mammalian cells at therapeutic concentrations and were shown to be inhibitors of parasitic
DHFR in a biochemical enzyme assay | en_US |
dc.language.iso | en | en_US |
dc.publisher | RSC | en_US |
dc.title | Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 10948724 - Lourens, Anna Catharina U. | |