Identification of dialkyl diacetylene diols with potent cancer chemopreventive activity
- Identification of dialkyl diacetylene diols with potent cancer chemopreventive activity
- 이창용; 윤지호; 강경수; 노주원; 신동윤
- dialkyl diacetylene diol; cancer chemoprevention; quinone reductase; Gymnaster koraiensis; detoxification
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 25, NO 18, 4020-4023
- An increasing importance of chemoprevention for controlling cancer risks prompted the discovery of new active cancer chemopreventive agents. In this study, we designed and synthesized substituted hexa-2,4-diyne-1,6-diols, more structurally simplified, tunable, and easily preparable than natural gymnasterkoreaynes, and evaluated their cancer chemopreventive activities by measuring concentration of doubling quinone reductase activity (CD), cell viability, and chemopreventive index (CI). Most of the diols exhibited good CD activity and low cytotoxicity. In particular, tetradeca-5,7-diyne-4,9-diol and 2-methyltetradeca-5,7-diyne-4,9-diol showed the best cancer chemopreventive activity, approximately equipotent to that of sulforaphane. And, by synthesizing optically active stereoisomers of selected active compounds, the effect of stereochemistry was also studied. Eventually, we produced a chemopreventive compound for in vivo study. (C) 2015 Published by Elsevier Ltd
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