Synthesis and antitumor activity of nitrogen-based thiocolchicine derivatives
- VernacularTitle:硫代秋水仙碱衍生物的合成和抗肿瘤活性
- Author:
Bin WANG
;
Xiandao PAN
;
Hongyan LIU
;
Jing YANG
;
Zhaoyun Lü
;
Jinghua ZHAO
- Publication Type:Journal Article
- Keywords:
colchicine;
thiocolchicine;
synthesis;
antitumor activity
- From:
Acta Pharmaceutica Sinica
2006;41(11):1057-1063
- CountryChina
- Language:Chinese
-
Abstract:
Aim To search for colchicine derivatives which have high efficacy and low toxicity. Methods Colchicine was firstly converted into thiocolchicine, and then it was hydrolyzed to get 7-(N-deacetylthiocolchicine). At last, 7-(N-deacetylthiocolchicine) was amidated to get the target compounds. The chemical structure of these new derivatives was confirmed with 1H NMR, IR, MS, and HR-MS. The cytotoxicity of the compounds was tested by MTT assay. Their in vivo antitumor activity was evaluated against mice tumor H22 and U14. Results Twelve thiocolchicine derivatives are new compounds. Conclusion In vitro antitumor activity has showed that some of these thiocolchicines possessed cytotoxic activity superior to colchicine. However, in vivo antitumor activity indicated that these derivatives have poor efficacy in mice.
