title: Discovery of a new class of cinnamyl-triazole as potent and selective inhibitors of aromatase (cytochrome P450 19A1).
abstract: Synthesis of a novel class of natural product inspired cinnamyl-containing 1,4,5-triazole and the potent inhibition of human aromatase (CYP 450 19A1) by select members is described. Structure-activity data generated provides insights into the requirements for potency particularly the inclusion of an aryl bromide or chloride residue as a keto-bioisostere.
authors.affiliation: Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4M1, Canada.
authors.forename: James
authors.initials: J
authors.lastname: McNulty
authors.affiliation: Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4M1, Canada.
authors.forename: Kunal
authors.initials: K
authors.lastname: Keskar
authors.affiliation: Department of Obstetrics and Gynecology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4K1, Canada.
authors.forename: Denis J
authors.initials: DJ
authors.lastname: Crankshaw
authors.affiliation: Department of Obstetrics and Gynecology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4K1, Canada.
authors.forename: Alison C
authors.initials: AC
authors.lastname: Holloway
mesh_terms: D001141:Aromatase / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002934:Cinnamates / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047072:Aromatase Inhibitors; D002934:Cinnamates; D014230:Triazoles; D001141:Aromatase
keywords: Anticancer agents; Aromatase; Huisgen cycloaddition; Triazoles; Vinyl ethers