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Systemic structure-activity relationship study of phenyl polyyne diols as potential chemopreventive agents
- Authors
- Lee, Chang-Yong; Shin, Dongyun
- Issue Date
- 15-Oct-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Anticancer; Chemoprevention; Quinone reductase; Gymnasterkoreayne
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.20, pp.4907 - 4910
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 26
- Number
- 20
- Start Page
- 4907
- End Page
- 4910
- ISSN
- 0960-894X
- Abstract
- The present study reports the cancer chemopreventive activities of phenyl polyyne diols derived from polyacetylene triol. Thirty-seven analogues based on a 1-phenylhexa-2,4-diyne-1,6-diol scaffold were prepared and their effects on QR activity were elucidated, as well as their cytotoxicities. We found that most of the derivatives based on phenylhexa-2,4-diyne-1,6-diol exhibited good QR induction activity and relatively low cytotoxicity and systemic structure-activity relationship was revealed. In particular, 4-fluorophenyl, 3-chlorophenyl, and 3,4-dioxolophenyl derivatives showed the best profiles in terms of QR induction, cytotoxicity, and CI. (C) 2016 Elsevier Ltd. All rights reserved.
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Related Researcher
- Shin, Dong Yun
- Pharmacy (Dept.of Pharmacy)