title: Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: an assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers.
abstract: A number of cytotoxic conjugated unsaturated ketones were screened for their membrane permeability characteristics using Caco-2 and MDCK cells with the view of finding promising leads for in vivo evaluations. 3b-e and 4a-b demonstrated high permeability characteristics. In particular, 4a emerged as a promising lead which showed excellent apparent permeability (P(app): 54.70) and efflux ratio (ER: 0.15) values. In general, the relative apparent permeabilities of these enones are similar in both bioassays.
authors.affiliation: Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada.
authors.forename: Ravi S P
authors.initials: RS
authors.lastname: Singh
authors.affiliation: Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada.
authors.forename: Deborah
authors.initials: D
authors.lastname: Michel
authors.affiliation: Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada.
authors.forename: Umashankar
authors.initials: U
authors.lastname: Das
authors.affiliation: Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada.
authors.forename: Jonathan R
authors.initials: JR
authors.lastname: Dimmock
authors.affiliation: Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada. Electronic address: jane.alcorn@usask.ca.
authors.forename: Jane
authors.initials: J
authors.lastname: Alcorn
mesh_terms: D000466:Alkadienes / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity*; D000818:Animals; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability / Q000187:drug effects* / Q000502:physiology; D003603:Cytotoxins / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity*; D004285:Dogs; D006801:Humans; D061985:Madin Darby Canine Kidney Cells; D013045:Species Specificity
chemical_list: D000466:Alkadienes; D003603:Cytotoxins
keywords: 4-Piperidones; Caco-2 cells; MDCK cells; Permeability; Unsaturated ketones