title: Synthesis and biological evaluation of novel symmetry bis-enediynes.
abstract: A series of acyclic symmetry bis-enediynes have been synthesized successfully and their bioactivities were evaluated. Among them, 1,6-bis(4-((2-(pyridin-2-ylethynyl)phenyl)ethynyl)phenoxy)hexane 8g showed good inhibition activity against the CCRF-CEM (GI(50)=0.04 microM) and HL-60 (GI(50)=0.09 microM) cell lines of human leukemia. The cell cycle analysis shows that compound 8g arrests cell cycle via inhibiting Cyclin A and Cyclin B expressions in low concentration and induces a significant apoptosis progress in high concentration.
authors.affiliation: Faculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
authors.forename: Kuo-Feng
authors.initials: KF
authors.lastname: Tseng
authors.forename: Chi-Fong
authors.initials: CF
authors.lastname: Lin
authors.forename: Yu-Hsiang
authors.initials: YH
authors.lastname: Lo
authors.forename: Yi-Ling
authors.initials: YL
authors.lastname: Hu
authors.forename: Li-Yi
authors.initials: LY
authors.lastname: Chen
authors.forename: Sheng-Huei
authors.initials: SH
authors.lastname: Yang
authors.forename: Shinne-Ren
authors.initials: SR
authors.lastname: Lin
authors.forename: Long-Sen
authors.initials: LS
authors.lastname: Chang
authors.forename: Ming-Jung
authors.initials: MJ
authors.lastname: Wu
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D019925:Cyclin A / Q000037:antagonists & inhibitors; D019926:Cyclin B / Q000037:antagonists & inhibitors; D004305:Dose-Response Relationship, Drug; D053281:Enediynes / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007938:Leukemia / Q000188:drug therapy* / Q000473:pathology
chemical_list: D019925:Cyclin A; D019926:Cyclin B; D053281:Enediynes