Systemic structure-activity relationship study of phenyl polyyne diols as potential chemopreventive agents.
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.
College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 21936, Republic of Korea. Electronic address: yonghana@hotmail.com.
Chang-Yong
CY
Lee
College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 21936, Republic of Korea. Electronic address: dyshin@gachon.ac.kr.
Dongyun
D
Shin
D016588:Anticarcinogenic Agents / Q000737:chemistry* / Q000494:pharmacology*; D053279:Polyynes / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D016588:Anticarcinogenic Agents; D053279:Polyynes
Anticancer; Chemoprevention; Gymnasterkoreayne; Quinone reductase