A series of 1,3-diaryl-2-propenones 2a-j and analogous 2-benzylidene-1,3-indandiones 3a-j were evaluated against various neoplasms and normal cells. In general, greater cytotoxic potencies and selective toxicity to human malignant cells were observed by the compounds in series 2 rather than 3. In particular, 2i emerged as a lead molecule having an average CC(50) figure of 8.6 µM and a selective index value of 18. Various physicochemical features of 2a-j were correlated with the cytotoxic potencies to neoplastic cell lines which provide guidelines for expansion of this series of compounds. The enone 2i induced internucleosomal DNA fragmentation and activated caspase-3 in HL-60 cells suggesting that one of the ways in which the cytotoxicity of the compounds in series 2 is mediated towards some of the cell lines used in this study is by apoptosis. Neurotoxicity in mice was generally lower in series 2 than 3a-j.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3327711PMC
http://dx.doi.org/10.1002/ardp.200900308DOI Listing

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