title: [Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives].
abstract: OBJECTIVE
  To improve the profile of 20 (S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed.
  
  
  METHODS
  These derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with 1HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by MTT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H22 in mice.
  
  
  RESULTS
  Twelve derivatives of camptothecin ester are new compounds.
  
  
  CONCLUSIONS
  In vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H22 mouse liver tumoral model.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. xdp@imm.ac.cn
authors.forename: Xian-dao
authors.initials: XD
authors.lastname: Pan
authors.forename: Hong-yan
authors.initials: HY
authors.lastname: Liu
authors.forename: Piao-yang
authors.initials: PY
authors.lastname: Sun
authors.forename: Cheng-gen
authors.initials: CG
authors.lastname: Zhu
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.forename: Kai-hong
authors.initials: KH
authors.lastname: Yuan
authors.forename: Rui
authors.initials: R
authors.lastname: Han
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D004952:Esters / Q000737:chemistry; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000473:pathology*; D051379:Mice; D008813:Mice, Inbred ICR; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D019772:Topotecan / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004952:Esters; C496393:topotecan-20-O-(4-fluorophenoxyacetate); D019772:Topotecan; D002166:Camptothecin