title: Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation.
abstract: A series of enmein-type diterpenoid analogs (11-20) derived from natural kaurene-type diterpenoid oridonin were synthesized and biologically evaluated. All target compounds showed improved anti-proliferative activities against four human cancer cell lines compared with natural oridonin and parent compound 10. Some compounds were more potent than positive control Taxol. Furthermore, mechanistic investigation showed that the representative compound 17 affected cell cycle and induced apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway.
authors: Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
authors: Dahong
authors: D
authors: Li
authors: Shengtao
authors: S
authors: Xu
authors: Hao
authors: H
authors: Cai
authors: Lingling
authors: L
authors: Pei
authors: Hengyuan
authors: H
authors: Zhang
authors: Lei
authors: L
authors: Wang
authors: Hequan
authors: H
authors: Yao
authors: Xiaoming
authors: X
authors: Wu
authors: Jieyun
authors: J
authors: Jiang
authors: Yijun
authors: Y
authors: Sun
authors: Jinyi
authors: J
authors: Xu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045786:Diterpenes, Kaurane / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004224:Diterpenes; D045786:Diterpenes, Kaurane; C011959:oridonin; C002627:kaurene; C007594:enmein