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논문 기본 정보

자료유형
학술저널
저자정보
Cho, Won-Jea (College of Pharmacy, Chonnam National University) Yoo, Su-Jeong (College of Pharmacy, Chonnam National University) Chung, Byung-Ho (College of Pharmacy, Chonnam National University) Choi, Bo-Gil (College of Pharmacy, Chonnam National University) Cheon, Seung-Hoon (College of Pharmacy, Chonnam National University) Whang, Soon-Ho (College of Pharmacy, KyungHee University) Kim, Sin-Kyu (College of Pharmacy, KyungHee University) Kang, Boo-Hyon (Screening and Toxicology Research Center, Korea Research Institute of Chemical Technology) Lee, Chong-Ock (Screening and Toxicology Research Center, Korea Research Institute of Chemical Technology)
저널정보
대한약학회 Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 제19권 제4호
발행연도
1996.1
수록면
321 - 325 (5page)

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Aiming at the development of anticancer agents by modification of phenolic benzo[c]phenanthridine alkaloid, additional hydroxyl group was put on C10 position of fagaridine (1) by a biomimetic synthetic procedure to afford 10-hydroxyfagaridine (12). All of the synthetic intermediates were also screened in vitro antitumor activities against five different cell lines as well as 12. Among them the representative cytotoxic results are shown as follows; P-quinone (11) $[ED_50;(A549=0.22; {\mu}g/ml)$, $(HCT;15=0.21 {\mu}g/ml)$, fagaridine (1) $(HCT;15=0.41 {\mu}g/ml)$, olefin (6) $(HCT; 15=0.06 {\mu}g/ml)$, acetal (7) $(SKMEL-2=0.07 {\mu}g/ml)$, dihydrofagaridne (10) $(A549=0.38 {\mu}g/ml)$, 10-hydroxyfagaridine (12) $(A 549=0.45{\mu}g/mi)$. From these observation three main remarks can be drawn; (i) the iminium part of benzo[c]phenanthridine is not essential for showing acitvities, (ii) the additional hydroxyl group did not contribute to enhance the cytotoxicity, (iii) the 3-arylisoquinolin-1(2H)-one derivatives were found to display significant in vitro antitumor activity.

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