title: Semisynthesis and antitumor activities of new styryl-lactone derivatives.
abstract: Nineteen new derivatives of the naturally occurring compound, goniothalamin, were prepared by chemical modification and semi-synthetic methods. The antitumor activities of these derivatives and goniothalamin were evaluated in vitro against human tumor cell lines, and most of them showed an inhibitory effect against HL-60 cancer cells. The derivatives 10-nitro-goniothalamin and 10-amino-goniothalamin gave selective inhibition concentration (IC50) of 1.10 and 1.14 microg/ml, respectively, against human stomach cancer SGC-7901 cells, while that of etoposide (vp-16) as the positive control was 6.07 microg/ml. Finally, the partition coefficients, logP (pi values), of these derivative molecules, were evaluated by calculating the additive approximate organic fragment logP value.
authors.affiliation: School of Pharmacy, Fudan University, Shanghai, China.
authors.forename: Fu Sheng
authors.initials: FS
authors.lastname: Zhou
authors.forename: Wei Dong
authors.initials: WD
authors.lastname: Tang
authors.forename: Qing
authors.initials: Q
authors.lastname: Mu
authors.forename: Guo Xun
authors.initials: GX
authors.lastname: Yang
authors.forename: Yang
authors.initials: Y
authors.lastname: Wang
authors.forename: Gao Lin
authors.initials: GL
authors.lastname: Liang
authors.forename: Li Guang
authors.initials: LG
authors.lastname: Lou
mesh_terms: D029061:Annonaceae / Q000737:chemistry*; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002855:Chromatography, Thin Layer; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D018515:Plant Leaves / Q000737:chemistry; D021241:Spectrometry, Mass, Electrospray Ionization; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013056:Spectrophotometry, Ultraviolet; D013343:Styrenes / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D007202:Indicators and Reagents; D007783:Lactones; D013343:Styrenes