Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bbrc.2009.07.104
Title: Structure-activity analysis of 2′-modified cinnamaldehyde analogues as potential anticancer agents
Authors: Gan, F.F. 
Chua, Y.S.
Hagen, T. 
Scarmagnani, S.
Palaniappan, P.
Westwell, A.D.
Franks, M.
Bradshaw, T.D.
Poobalasingam, T.
Keywords: Anticancer drugs
Apoptosis
Cinnamaldehydes
Michael acceptors
Structure-activity analysis
Issue Date: 2009
Source: Gan, F.F., Chua, Y.S., Hagen, T., Scarmagnani, S., Palaniappan, P., Westwell, A.D., Franks, M., Bradshaw, T.D., Poobalasingam, T. (2009). Structure-activity analysis of 2′-modified cinnamaldehyde analogues as potential anticancer agents. Biochemical and Biophysical Research Communications 387 (4) : 741-747. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bbrc.2009.07.104
Abstract: The natural product 2′-hydroxycinnamaldehyde (HCA) and its analogue, 2′-benzoyloxycinnamaldehyde (BCA), have been previously shown to have antiproliferative and proapoptotic effects in vitro and inhibit tumor growth in vivo. In this study, we use structure-activity analysis to define structural features that are important for the activity of cinnamaldehyde analogues. Our results emphasize an important role for both the propenal group as well as the modification at the 2′-position. Further studies were aimed to characterize the mechanism of action of BCA. Exposure to BCA induced cell death via caspase-dependent and -independent pathways. Cell death was not due to autophagy or necrosis as a result of energy depletion or induction of reactive oxygen species. Our findings have important implications for future drug design and highlight the importance of defining molecular drug targets for this promising class of potential anticancer agents. © 2009 Elsevier Inc. All rights reserved.
Source Title: Biochemical and Biophysical Research Communications
URI: http://scholarbank.nus.edu.sg/handle/10635/28660
ISSN: 0006291X
10902104
DOI: 10.1016/j.bbrc.2009.07.104
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