title: Synthesis, anti-tumor activity, and structure-activity relationships of curcumol derivatives.
abstract: Using curcumol that was extracted from the volatile oil of Rhizoma Curcumae as the raw material, its derivatives were synthesized and purified. The structures of these compounds were confirmed by (1)H, (13)C NMR, and mass spectral data. The test compounds were evaluated for their in vitro anti-tumor activity against gastric cancer cell lines SGC-7901 and lung carcinoma cell line H460 by methyl thiazolyl tetrazolium chromatometry. Distinct structure-activity relationships of these curcumol derivatives were also revealed for inhibiting cell proliferation. Presence of electron-withdrawing groups or amino could increase the activity significantly, whereas esterification of 8-hydroxy diminished the anti-tumor activity. Many of the tested candidates exhibited higher inhibition efficiency than curcumol, suggesting that structural modifications could enhance its activity effectively.
authors.affiliation: a Institute of Chemical Technology, Nanjing University of Science and Technology , Nanjing , 210094 , China.
authors.forename: Ping
authors.initials: P
authors.lastname: Guo
authors.forename: Yue-Wu
authors.initials: YW
authors.lastname: Wang
authors.forename: Bi-Xia
authors.initials: BX
authors.lastname: Weng
authors.forename: Xiao-Kun
authors.initials: XK
authors.lastname: Li
authors.forename: Shu-Lin
authors.initials: SL
authors.lastname: Yang
authors.forename: Fa-Qing
authors.initials: FQ
authors.lastname: Ye
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms; D019906:Nuclear Magnetic Resonance, Biomolecular; D027343:Rhizome; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D012717:Sesquiterpenes; C022801:curcumol