Citation: Di Zao Li, Yan Li, Xiao Guang Chen, Chen Gen Zhu, Jing Yang, Hong Yan Liu, Xian Dao Pan. Synthesis and antitumor activity of heterocyclic acid ester derivatives of 20S-camptothecins[J]. Chinese Chemical Letters, ;2007, 18(11): 1335-1338. doi: 10.1016/j.cclet.2007.09.014 shu

Synthesis and antitumor activity of heterocyclic acid ester derivatives of 20S-camptothecins

Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

Received Date: 14 June 2007

A series of heterocyclic acid esters of camptothecins as new compounds had been synthesized by acylation method, their in vitro and in vivo antitumor activities were evaluated. The cytotoxic results showed that 6 possessed the best efficacy on six human cancer cell lines in the six classes of CPTs' derivatives. In vivo testing results indicated that 9 had better antitumor activity against mouse liver carcinoma H₂₂ than topotecan.
- Camptothecin,
- Synthesis,
- Heterocyclic acid,
- Antitumor activity
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