title: Synthesis and antitumor activity of nitrogen-based thiocolchicine derivatives.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Wang
authors.forename: Xian-dao
authors.initials: XD
authors.lastname: Pan
authors.forename: Hong-yan
authors.initials: HY
authors.lastname: Liu
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.forename: Zhao-yun
authors.initials: ZY
authors.lastname: Lü
authors.forename: Jing-hua
authors.initials: JH
authors.lastname: Zhao
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003078:Colchicine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008114:Liver Neoplasms, Experimental / Q000473:pathology / Q000517:prevention & control*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008956:Models, Chemical; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D011471:Prostatic Neoplasms / Q000473:pathology / Q000517:prevention & control*; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; C014856:thiocholchicine; D003078:Colchicine