Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 22, Pages 5199-5202Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.074
Keywords
Unsaturated ketones; Caco-2 cells; MDCK cells; Permeability; 4-Piperidones
Categories
Funding
- Canadian Institutes of Health Research
- Industry Liaison Office of the University of Saskatchewan
- College of Graduate Studies and Research, University of Saskatchewan
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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. (C) 2014 Elsevier Ltd. All rights reserved.
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