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  • Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.

Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.

European journal of medicinal chemistry (2017-02-22)
Neill J Horley, Kenneth J M Beresford, Tarun Chawla, Glen J P McCann, Ketan C Ruparelia, Linda Gatchie, Vinay R Sonawane, Ibidapo S Williams, Hoon L Tan, Prashant Joshi, Sonali S Bharate, Vikas Kumar, Sandip B Bharate, Bhabatosh Chaudhuri
ABSTRACT

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 inhibit human CYP1B1 enzyme bound to yeast-derived microsomes (Sacchrosomes™) with IC

MATERIALS
Product Number
Brand
Product Description

SAFC
MEM Non-essential Amino Acid Solution (100×), without L-glutamine, liquid, sterile-filtered, BioReagent, suitable for cell culture
Sigma-Aldrich
L-(−)-Glucose, ≥99%