Synthesis and antitrypanosomal activities of novel pyridylchalcones

Eur J Med Chem. 2017 Mar 10:128:213-218. doi: 10.1016/j.ejmech.2017.01.027.

Avninder S Bhambra ¹, Ketan C Ruparelia ², Hoon L Tan ², Deniz Tasdemir ³, Hollie Burrell-Saward ⁴, Vanessa Yardley ⁴, Kenneth J M Beresford ⁵, Randolph R J Arroo ²

Affiliations

1 School of Allied Health Sciences, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
2 Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
3 GEOMAR Centre for Marine Biotechnology, Research Unit Marine Natural Products Chemistry, GEOMAR Helmholtz Centre for Ocean Research Kiel, Am Kiel-Kanal 44, D-24106, Kiel, Germany.
4 Faculty of Infectious and Tropical Disease, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, UK.
5 Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK. Electronic address: kberesford@dmu.ac.uk.

PMID: 28189085 DOI: 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).

Keywords

Claisen-Schmidt; Leishmania donovani; Neglected tropical disease; Pyridylchalcone; Trypanosoma brucei rhodesiense.

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