title: Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents.
abstract: A series of novel 1,2,3-triazole-pyrimidine hybrids were designed, synthesized and evaluated for their anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Compound 17 showed the most excellent anticancer activity with single-digit micromolar IC50 values ranging from 1.42 to 6.52 μM. Further mechanism studies revealed that compound 17 could obviously inhibit the proliferation of EC-109 cancer cells by inducing apoptosis and arresting the cell cycle at G2/M phase.
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Li-Ying
authors.initials: LY
authors.lastname: Ma
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Lu-Ping
authors.initials: LP
authors.lastname: Pang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Miao
authors.initials: M
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Biao
authors.initials: B
authors.lastname: Hu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Deng-Qi
authors.initials: DQ
authors.lastname: Xue
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Kun-Peng
authors.initials: KP
authors.lastname: Shao
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Bao-Le
authors.initials: BL
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors.forename: En
authors.initials: E
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR 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*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines; D014230:Triazoles; C030986:pyrimidine
keywords: Anticancer; Apoptosis; Cell cycle arrest; Pyrimidine; Triazole