title: Design, synthesis, and antitumor activity of novel acylate of 6-OH at 1- O-acetylbritannilactone.
abstract: N-(α-Alkyloxime-3-phenylpropionyl) proline was designed and synthesized as an acylating agent to modify the 6-OH of 1-O-acetylbritannilactone. Eight intermediates and eight target compounds were obtained. The structures of sixteen novel compounds were characterized by (1)HNMR, IR and HRMS. The activities against HL-60 and Bel-7402 cell lines were tested, the IC50 values of compound IVg were 2.7 μM and 4.3 μM, respectively.
authors.forename: Shouxin
authors.initials: S
authors.lastname: Liu
authors.forename: Jun
authors.initials: J
authors.lastname: Feng
authors.forename: He
authors.initials: H
authors.lastname: Liu
authors.forename: Junzhang
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory Breeding Base, Hebei Laboratory of Molecular Chemistry for Drug, College of Chemical and Pharmaceutical Engineering, Hebei University of Science & Technology, Shijiazhuang 050018, P.R. China. chlsx@hebust.edu.cn.
authors.forename: Xia
authors.initials: X
authors.lastname: Tian
mesh_terms: D000215:Acylation; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D018922:HL-60 Cells; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007783:Lactones; C500401:O-acetylbritaanilactone; D012717:Sesquiterpenes