Synthesis and antiprotozoal activity of 4-arylcoumarins.
A large series of 4-arylcoumarins was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiprotozoal activity against Plasmodium falciparum and Leishmania donovani. Several compounds were found to strongly inhibit the proliferation of human cell line and/or parasites. The 4-(3,4-dimethoxyphenyl)-6,7-dimethoxycoumarin exhibit a potent activity on L. donovani amastigotes with a selectivity index (SI=265) twice than amphotericin B (SI=140).
Pierson
Jean-Thomas
JT
Faculté des Sciences de Saint-Jérôme, UMR-CNRS 6264, Laboratoire Chimie Provence, Universités Aix-Marseille I, II and III, 13397 Marseille Cedex 20, France.
Dumètre
Aurélien
A
Hutter
Sébastien
S
Delmas
Florence
F
Laget
Michèle
M
Finet
Jean-Pierre
JP
Azas
Nadine
N
Combes
Sébastien
S
D015110:4-Hydroxycoumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000666:Amphotericin B / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*
C550192:4-(3,4-dimethoxyphenyl)-6,7-dimethoxycoumarin; D015110:4-Hydroxycoumarins; D000981:Antiprotozoal Agents; D003374:Coumarins; D010165:Palladium; D000666:Amphotericin B