Synthesis and in vitro biological activity of chalcone derivatives as potential antiparasitic agents
Koketso J. Setshedi, Richard M. Beteck, Kayhan Ilbeigi, Dorien Mabille, Guy Caljon, Lesetja J. Legoabe
Abstract
Abstract Kinetoplastids are a group of flagellated protozoans including medically important parasites of the genus Trypanosoma and Leishmania . The corresponding diseases have afflicted humans for centuries. In an effort to combat kinetoplastid infections, a set of 21 chalcones was synthesized and evaluated for their in vitro anti-protozoal efficacy against Trypanosoma brucei , Trypanosoma brucei rhodesiense , Trypanosoma cruzi , and Leishmania infantum . To ensure safety, these compounds underwent a selectivity evaluation by assessing toxicity against a human lung fibroblast cell line. Compound K4 exhibited remarkable and selective trypanocidal activity against T. b. brucei with IC 50 value of 0.31 ± 0.27 µM and T. b. rhodesiense with IC 50 value of 0.96 ± 0.86 µM. Compound K9 also showed significant trypanocidal activity against T. b. brucei (IC 50 : 0.45 ± 0.14 µM) and T. b. rhodesiense (IC 50 : 0.93 ± 0.51 µM). In both compounds, electron withdrawing groups are appended to the styrenyl moiety.