title: Synthesis and anticancer activity of novel C6-piperazine substituted purine steroid-nucleosides analogues.
abstract: Novel C6-piperazine substituted purine nucleoside analogues (2-9) bearing a modified pyranose-like D ring of the 4-azasteroid moiety were efficiently synthesized through nucleophilic substitution at C6 position of the steroid-nucleoside precursors (1) with versatile piperazines. All newly-synthesized compounds were evaluated for their anticancer activity in vitro against Hela, PC-3 and MCF-7 cell lines. Among them, compounds 8b and 9b exhibited significant cytotoxicity on PC-3 cell lines.
authors.affiliation: College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Li-Hua
authors.initials: LH
authors.lastname: Huang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Hong-De
authors.initials: HD
authors.lastname: Xu
authors.affiliation: College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Zhuo-Ya
authors.initials: ZY
authors.lastname: Yang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Yong-Fei
authors.initials: YF
authors.lastname: Zheng
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China. Electronic address: liuhm@zzu.edu.cn.
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D008968:Molecular Conformation; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009705:Nucleosides; D010879:Piperazines; D011687:Purines; D013256:Steroids; D000077489:Piperazine; C030985:purine
keywords: Anticancer activity; Nucleoside analogues; Nucleosides; Piperazines; Purine