Synthesis of benzo[c]phenanthridine derivatives and theirin vitro antitumor activities |
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Authors: | Won-Jea Cho Su-Jeong Yoo Byung-Ho Chung Bo-Gil Choi Seung Hoon Cheon Soon-Ho Whang Sin-Kyu Kim Boo-Hyon Kang Chong-Ock Lee |
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Institution: | 1. College of Pharmacy, Chonnam National University, YongBong-dong, Buk-gu, 500-757, Kwanju, Korea 2. College of Pharmacy, KyungHee University, 130-701, Seoul, Korea 3. Screening & Toxicology Research Center, Korea Research Institute of Chemical Technology, 305-606, Daejeon, Korea
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Abstract: | Aiming at the development of anticancer agents by modification of phenolic benzoc]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 screenedin vitro antitumor activities against five different cell lines as well as12. Among them the representative cytotoxic results are shown as follows;p-quinone (11) ED50 (A549=0.22 μg/ml), (HCT15=0.21 μg/ml), fagaridine (1) (HCT 15=0.41 μg/ml), olefin (6) (HCT 15=0.06 μg/ml), acetal (7) (SKMEL-2=0.07 μg/ml), dihydrofagaridne (10) (A549=0. 38 μg/ml), 10-hydroxyfagaridine (12) (A 549=0.45 μg/ml). From these observation three main remarks can be drawn; (i) the iminium part of benzoc]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 significantin vitro antitumor activity. |
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