Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: An assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers

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.