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 J.M. and Arroo, Randolph R.J. (2017) Synthesis and antitrypanosomal activities of novel pyridylchalcones. European Journal of Medicinal Chemistry, 128 . pp. 213-218. DOI 10.1016/j.ejmech.2017.01.027.

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Supplementary data:

Abstract

Highlights:
• Improved Claisen-Schmidt condensation using lithium hydroxide monohydrate in 1,4-dioxane.
• Pyridylchalcones show good activity and selectivity against Trypanosoma brucei.
• Pyridylchalcones show little activity against Leishmania donovani.
• Promising leads in the development of novel compounds for the treatment of sleeping sickness.
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).

Document Type: Article
Keywords: Neglected tropical disease; Trypanosoma brucei rhodesiense; Leishmania donovani; Pyridylchalcone; Claisen-Schmidt
Research affiliation: OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MN Marine natural products chemistry
Refereed: Yes
Open Access Journal?: No
DOI etc.: 10.1016/j.ejmech.2017.01.027
ISSN: 0223-5234
Projects: Future Ocean
Date Deposited: 28 Feb 2017 14:17
Last Modified: 01 Feb 2019 15:11
URI: http://oceanrep.geomar.de/id/eprint/36726

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