Citation: 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. doi: 10.1016/j.cclet.2008.05.042 shu

Synthesis and antitumor activity of 9-methyl-10-hydroxycamptothecin

Department of Medicinal Chemistry, China. Pharmaceutical University, Nanjing 210009, China

Received Date: 24 March 2008

Fund Project: China (No.BK2007168)This work was supported by the Natural Science Foundation of Jiangsu Province

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.
- Synthesis,
- Camptothecin,
- 1O-Hydroxycamptothecin,
- Cytotoxicity
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