Synthesis and antitumor activity of nitrogen-based thiocolchicine derivatives / 药学学报

ABSTRACT

<p><b>AIM</b>To search for colchicine derivatives which have high efficacy and low toxicity.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>Twelve thiocolchicine derivatives are new compounds.</p><p><b>CONCLUSION</b>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.</p>