title: Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates.
abstract: Novel 1-O- and 14-O-derivatives of oridonin were synthesized and biologically evaluated. All of the derivatives exhibited stronger cytotoxicity against six cancer cell lines (BGC-7901, SW-480, HL-60, BEL-7402, A549, and B16) than oridonin in vitro, and some of them were more potent than oridonin and cyclophosphamide in vivo. Compounds Ib and IIg were the most potent with the IC(50) values of 0.84 microM for Ib in HL-60 cell and 1.00 microM for IIg in BEL-7402 cell.
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing 210009, China. jinyixu@china.com
authors.forename: Jinyi
authors.initials: J
authors.lastname: Xu
authors.forename: Jingyi
authors.initials: J
authors.lastname: Yang
authors.forename: Qian
authors.initials: Q
authors.lastname: Ran
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.forename: Zhixuan
authors.initials: Z
authors.lastname: Wang
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Wu
authors.forename: Weiyi
authors.initials: W
authors.lastname: Hua
authors.forename: Shengtao
authors.initials: S
authors.lastname: Yuan
authors.forename: Luyong
authors.initials: L
authors.lastname: Zhang
authors.forename: Mingqin
authors.initials: M
authors.lastname: Shen
authors.forename: Yongfang
authors.initials: Y
authors.lastname: Ding
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D045786:Diterpenes, Kaurane / Q000737:chemistry* / Q000302:isolation & purification*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000138:chemical synthesis / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D045786:Diterpenes, Kaurane; D013778:Tetrazolium Salts; D013844:Thiazoles; C011959:oridonin; C022616:thiazolyl blue; D005472:Fluorouracil