| Synthesis and antitumor activity of 9-methyl-10-hydroxycamptothecin |
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| 作者姓名： | Sheng Wang Yu Yan Li Qi Dong You |
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| 作者单位： | Department of Medicinal Chemistry, China. Pharmaceutical University, Nanjing 210009, China |
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| 摘 要： | A novel camptothecin analogue, 9-methyl-10-hydroxycamptothecin （4）, was unexpectedly synthesized from 10-hydroxycamptothecin in two steps. The key step included an efficient Mannich-type reaction. The overall yield was 47.2%. An ether analogue of 4, 9-methyl-10-benzylaminomethoxycamptothecin （5）, was also prepared. These new camptothecin analogues were evaluated for in vitro cytotoxicity against four human cancer cell lines, and exhibited more potent antitumor activities than contrals camptothecin and topotecan against several cancer cells.
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| 关 键 词： | 喜树碱 合成方法 10-羟基尿素 细胞毒性 |
| 收稿时间： | 24 March 2008 |
Synthesis and antitumor activity of 9-methyl-10-hydroxycamptothecin |
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| Sheng Wang,Yu Yan Li,Qi Dong You.Synthesis and antitumor activity of 9-methyl-10-hydroxycamptothecin[J].Chinese Chemical Letters,2008,19(8):918-920. |
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| Authors: | Sheng Wang Yu Yan Li Qi Dong You |
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| Institution: | Department of Medicinal Chemistry, China. Pharmaceutical University, Nanjing 210009, China |
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| Abstract: | A novel camptothecin analogue, 9-methyl-10-hydroxycamptothecin (4), was unexpectedly synthesized from 10-hydroxycamptothecin in two steps. The key step included an efficient Mannich-type reaction. The overall yield was 47.2%. An ether analogue of 4, 9-methyl-10-benzylaminomethoxycamptothecin (5), was also prepared. These new camptothecin analogues were evaluated for in vitro cytotoxicity against four human cancer cell lines, and exhibited more potent antitumor activities than contrals camptothecin and topotecan against several cancer cells. |
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| Keywords: | Synthesis Camptothecin 1O-Hydroxycamptothecin Cytotoxicity |
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