title: Design and synthesis of new tetrandrine derivatives and their antitumor activities.
abstract: A series of tetrandrine derivatives were designed and synthesized using Suzuki coupling reaction. Eleven targeted compounds with over 50% inhibition against HL60 and A549 human cancer cell lines at 10 μM were further evaluated for the in vitro antitumor activities by MTT or SRB assay. The biological results revealed that some compounds exhibited potent antitumor activities. Thiophene derivative 6 and acetylphenyl derivative 5 were the most active ones against HL60 and A549 cell lines, with IC50 values less than 5 μM, which thus could be considered as useful candidate for further development of new antitumor agents.
authors.affiliation: a School of Pharmaceutical Science , Shanxi Medical University , Taiyuan 030001 , China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Wei
authors.affiliation: a School of Pharmaceutical Science , Shanxi Medical University , Taiyuan 030001 , China.
authors.forename: Ting-Li
authors.initials: TL
authors.lastname: Qu
authors.affiliation: b Shanghai Institute of Pharmaceutical Industry , Shanghai 200040 , China.
authors.forename: Yi-Fang
authors.initials: YF
authors.lastname: Yang
authors.affiliation: a School of Pharmaceutical Science , Shanxi Medical University , Taiyuan 030001 , China.
authors.forename: Jin-Fang
authors.initials: JF
authors.lastname: Xu
authors.affiliation: c State Key Laboratory of New Drug Research , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
authors.forename: Xu-Wen
authors.initials: XW
authors.lastname: Li
authors.affiliation: a School of Pharmaceutical Science , Shanxi Medical University , Taiyuan 030001 , China.
authors.forename: Zheng-Bao
authors.initials: ZB
authors.lastname: Zhao
authors.affiliation: c State Key Laboratory of New Drug Research , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
authors.forename: Yue-Wei
authors.initials: YW
authors.lastname: Guo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D044182:Benzylisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D044182:Benzylisoquinolines; C009438:tetrandrine
keywords: Suzuki coupling; Tetrandrine; antitumor activity; structure–activity relationship; synthesis