Identification of dialkyl diacetylene diols with potent cancer chemopreventive activity

Title
Identification of dialkyl diacetylene diols with potent cancer chemopreventive activity
Authors
이창용윤지호강경수노주원신동윤
Keywords
dialkyl diacetylene diol; cancer chemoprevention; quinone reductase; Gymnaster koraiensis; detoxification
Issue Date
2015-09
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 25, NO 18, 4020-4023
Abstract
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
URI
http://pubs.kist.re.kr/handle/201004/50545
ISSN
0960894X
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