title: Synthesis and antitrypanosomal activities of novel pyridylchalcones.
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 IC50value 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).
authors.affiliation: School of Allied Health Sciences, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
authors.forename: Avninder S
authors.initials: AS
authors.lastname: Bhambra
authors.affiliation: Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
authors.forename: Ketan C
authors.initials: KC
authors.lastname: Ruparelia
authors.affiliation: Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
authors.forename: Hoon L
authors.initials: HL
authors.lastname: Tan
authors.affiliation: 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.
authors.forename: Deniz
authors.initials: D
authors.lastname: Tasdemir
authors.affiliation: Faculty of Infectious and Tropical Disease, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, UK.
authors.forename: Hollie
authors.initials: H
authors.lastname: Burrell-Saward
authors.affiliation: Faculty of Infectious and Tropical Disease, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, UK.
authors.forename: Vanessa
authors.initials: V
authors.lastname: Yardley
authors.affiliation: 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.
authors.forename: Kenneth J M
authors.initials: KJM
authors.lastname: Beresford
authors.affiliation: Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
authors.forename: Randolph R J
authors.initials: RRJ
authors.lastname: Arroo
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D014355:Chagas Disease / Q000188:drug therapy* / Q000469:parasitology; D047188:Chalcones / Q000737:chemistry*; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects; D007898:Leishmaniasis, Visceral / Q000188:drug therapy / Q000469:parasitology; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011407:Propane / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: C000617034:1-(3-bromophenyl)-3-(3-pyridinyl)prop-2-en-1-one; D047188:Chalcones; D011725:Pyridines; D014344:Trypanocidal Agents; D011407:Propane
keywords: Claisen-Schmidt; Leishmania donovani; Neglected tropical disease; Pyridylchalcone; Trypanosoma brucei rhodesiense