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• W2169595087 abstract "In the course of our search for new protein farnesyltransferase inhibitors with antiparasitic activity, we found that addition of a methionine residue at position 2 of 3-arylthiophenes greatly improved enzyme inhibition. To investigate the influence of this methionine residue on FTase and antiparasitic activities, 29 novel tetrasubstituted thiophenes bearing methionine or analogous moieties were synthesised. These new derivatives were evaluated on human and Trypanosoma brucei protein farnesyltransferases and on proliferation of 4 protozoan parasites: Plasmodium falciparum, Trypanosoma brucei brucei, Trypanosoma cruzi and Leishmania donovani. Some compounds showed promising low micromolar or submicromolar activities on T. b. brucei and L. donovani confirming the potential of this new class as antiparasitic agents." @default.
• W2169595087 created "2016-06-24" @default.
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• W2169595087 date "2013-01-01" @default.
• W2169595087 modified "2023-09-25" @default.
• W2169595087 title "Introduction of methionine mimics on 3-arylthiophene: influence on protein farnesyltransferase inhibition and on antiparasitic activity" @default.
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• W2169595087 doi "https://doi.org/10.1039/c3md00065f" @default.
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