TY - JOUR
T1 - 2-Arylpaullones are selective antitrypanosomal agents
AU - Ryczak, Jasmin
AU - Papini, Ma'ayan
AU - Lader, Annette
AU - Nasereddin, Abedelmajeed
AU - Kopelyanskiy, Dmitry
AU - Preu, Lutz
AU - Jaffe, Charles L.
AU - Kunick, Conrad
PY - 2013
Y1 - 2013
N2 - Antileishmanial paullone-chalcone hybrid molecules display antiparasitic activity against Trypanosoma brucei rhodesiense blood stream forms, albeit with low selectivity against human THP-1 cells. In order to develop less toxic analogues, paullones with acrylamide or aryl substituents in 2-position were synthesized, of which the latter exhibited potent antiparasitic activity with excellent selectivity profiles. The most potent compound identified in this study was 9-tert-butyl-2-(4-morpholinophenyl)paullone (3i) which inhibited the parasites at submicromolar concentrations (GI50 = 510 nM) with a selectivity index of 157.
AB - Antileishmanial paullone-chalcone hybrid molecules display antiparasitic activity against Trypanosoma brucei rhodesiense blood stream forms, albeit with low selectivity against human THP-1 cells. In order to develop less toxic analogues, paullones with acrylamide or aryl substituents in 2-position were synthesized, of which the latter exhibited potent antiparasitic activity with excellent selectivity profiles. The most potent compound identified in this study was 9-tert-butyl-2-(4-morpholinophenyl)paullone (3i) which inhibited the parasites at submicromolar concentrations (GI50 = 510 nM) with a selectivity index of 157.
KW - Neglected tropical diseases
KW - Paullones
KW - Suzuki reaction
KW - Trypanosoma brucei rhodesiense
KW - Trypanosomiasis
UR - http://www.scopus.com/inward/record.url?scp=84877028315&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2013.03.065
DO - 10.1016/j.ejmech.2013.03.065
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C2 - 23648975
AN - SCOPUS:84877028315
SN - 0223-5234
VL - 64
SP - 396
EP - 400
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -