title: Synthesis of novel spin-labeled podophyllotoxin derivatives as potential antineoplastic agents: Part XXV.
abstract: A series of novel spin-labeled 4β-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin derivatives (17a-h) were firstly designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed click approach, and evaluated for cytotoxicity against four human tumor cell lines (A-549, DU145, KB, and KBvin). Among them, compound17hdisplayed the highest cytotoxic activity against the tumor cell lines tested. Significantly, compound17hshowed superior cytotoxic activity compared with etoposide (IC506.30 to>10 μM), a clinically available anticancer drug. Significant activity toward the drug resistant KBvin cell line revealed promising future for compound17has a new generation of epipodophyllotoxin-derived antitumor clinical trial candidate.
authors.affiliation: Environmental and Municipal Engineering School, Lanzhou, Jiaotong University, Lanzhou 730000, People's Republic of China.
authors.forename: Liu
authors.initials: L
authors.lastname: Yang
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Nan
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Wen-Qun
authors.initials: WQ
authors.lastname: Li
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Mei-Juan
authors.initials: MJ
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Xiao-Bo
authors.initials: XB
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Ying-Qian
authors.initials: YQ
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
authors.forename: Zhi-Jun
authors.initials: ZJ
authors.lastname: Zhang
authors.affiliation: Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
authors.forename: Kuo-Hsiung
authors.initials: KH
authors.lastname: Lee
keywords: Click chemistry; Cytotoxic activity; Podophyllotoxin; Spin-labeled