Authors
H Hameed1; H P Price3; R Nash2; P D Horrocks1;
1 Institute for Science and Technology in Medicine, Keele University; 2 Phytoquest Limited; 3 School of Life Sciences, Keele University
Discussion
There is an urgent need to identify and evaluate novel chemical scaffolds to seed the drug discovery pipeline for parasitic diseases. The UK-based SME PhytoQuest has produced a library of about 1000 molecules representing a unique resource for lead discovery of high value chemicals from temperate zone plants. The library comprises pure compounds selected from a wide range of chemical classes, with a high degree of functionality and physiochemical properties that match Lipinski’s Rule of Five. A subset of 650 compounds have been screened against axenic amastigotes of Leishmania mexicana, bloodstream form Trypanosoma brucei and the intraerythrocytic stages of Plasmodium falciparum. Here we report a characterization of our hits against L. mexicana and T. brucei, with additional testing of selected compounds on L. donovani and human cell lines (THP-1 and HepG2).