title: Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: inhibitors of leukotriene B4.
abstract: A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B4 inhibitory activity using human whole blood assay (HWBL) afforded a lead compound, 1-(6-butoxy-2-naphthyl)-3-(4-nitrophenyl)-prop-2-en-1-one (K4A3) with an IC50 value of 18.5 microM.
authors.affiliation: Division of Organic Chemistry (Synthesis), National Chemical Laboratory, Pune, India.
authors.forename: A M
authors.initials: AM
authors.lastname: Deshpande
authors.forename: N P
authors.initials: NP
authors.lastname: Argade
authors.forename: A A
authors.initials: AA
authors.lastname: Natu
authors.forename: J
authors.initials: J
authors.lastname: Eckman
mesh_terms: D002599:Chalcone / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020024:Leukotriene Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009281:Naphthalenes / Q000737:chemistry
chemical_list: D020024:Leukotriene Antagonists; D009281:Naphthalenes; D007975:Leukotriene B4; C031721:naphthalene; D002599:Chalcone