Synthesis and antitrypanosomal activities of novel pyridylchalcones.

Bhambra, Avninder S; Ruparelia, Ketan C; Tan, Hoon L; Tasdemir, Deniz; Burrell-Saward, Hollie; Yardley, Vanessa; Beresford, Kenneth JM; Arroo, Randolph RJ; (2017) Synthesis and antitrypanosomal activities of novel pyridylchalcones. European journal of medicinal chemistry, 128. pp. 213-218. ISSN 0223-5234 DOI: https://doi.org/10.1016/j.ejmech.2017.01.027

Abstract

A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50 value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).