title: Synthesis, physicochemical characterization and pharmacological investigation of indolacin-5-fluorouracil-1-ylmethyl ester.
abstract: The objective of this work is to synthesize indolacin-5-fluorouracil-1-ylmethyl ester and the structure was confirmed by means of UV, IR,1H-NMR,13C-NMR and mass spectrometry. The physicochemical parameters of melting point, solubility, apparent partition coefficient were investigated. S180 sarcoma, H22 hapatitic cancer and Lewis-transplanted mice were used to evaluate the anti-tumor activity of indolacini-5-fluorouracil-1-ylmethyl ester compared with 5-fluorouracil in vivo. Anti-inflammatory and analgesic activities were evaluated in mice. The inhibitory ratio of indolacini- 5-fluorouracil-1-ylmethyl ester is comparative to that of 5-fluorouracil. This study indicates that 5-fluorouracil-1-ylmethyl ester may represent a new anticancer predrug of 5-fluorouracil to produce a combined effect of indolacin and 5-fluorouracil for cancer therapy.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China.
authors.forename: Mei-Juan
authors.initials: MJ
authors.lastname: Zou
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Chen
authors.affiliation: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road, Shenyang, China.
authors.forename: Yi-Ling
authors.initials: YL
authors.lastname: Sheng
authors.affiliation: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road, Shenyang, China.
authors.forename: Xiao-Mian
authors.initials: XM
authors.lastname: Zhou
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China.
authors.forename: Xiang-Rong
authors.initials: XR
authors.lastname: Zhang
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007210:Indoleacetic Acids / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D066244:Proton Magnetic Resonance Spectroscopy; D012510:Sarcoma 180 / Q000188:drug therapy* / Q000473:pathology; D012995:Solubility; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D044366:Transition Temperature; D047368:Tumor Burden / Q000187:drug effects
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000964:Antimetabolites, Antineoplastic; D007210:Indoleacetic Acids; C000620432:indolacin 5-fluorouracil-1-ylmethyl ester; D005472:Fluorouracil