878581-46-5Relevant articles and documents
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.,Arroo, Randolph R.J.
, p. 213 - 218 (2017/02/15)
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).
Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines
Horley, Neill J.,Beresford, Kenneth J.M.,Chawla, Tarun,McCann, Glen J.P.,Ruparelia, Ketan C.,Gatchie, Linda,Sonawane, Vinay R.,Williams, Ibidapo S.,Tan, Hoon L.,Joshi, Prashant,Bharate, Sonali S.,Kumar, Vikas,Bharate, Sandip B.,Chaudhuri, Bhabatosh
, p. 159 - 174 (2017/02/23)
The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inh
