title: Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives.
abstract: Trying to develop potent and selective anticancer agents, two series of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives were designed and synthesized. Their antitumor activities were evaluated by MTT method against four selected human cancer cell lines (MGC-803, EC-9706, HeLa and MCF-7). Our results showed that compound 11h exhibited good anticancer activities compared to 5-fluorouracil against the four tested cell lines, with IC50 values ranging from 2.0 to 4.5 μM. Flow cytometry analysis indicated that compound 11h induced the cellular early apoptosis and cell cycle arrest at G2/M phase in EC-9706.
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, 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, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Xu-Yao
authors.initials: XY
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Chao-Jie
authors.initials: CJ
authors.lastname: Wang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, 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, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Nan
authors.initials: N
authors.lastname: Zhu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Peng
authors.initials: P
authors.lastname: He
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, 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, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Peng-Ju
authors.initials: PJ
authors.lastname: Chen
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Yi-Fei
authors.initials: YF
authors.lastname: Gu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Xiao-Song
authors.initials: XS
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Cai-Feng
authors.initials: CF
authors.lastname: Wang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
authors.forename: Cong-Hui
authors.initials: CH
authors.lastname: Ji
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China. Electronic address: zqr406@sina.com.
authors.forename: Qiu-Rong
authors.initials: QR
authors.lastname: Zhang
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, 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*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D010793:Phthalazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D010793:Phthalazines; D014230:Triazoles; C043388:phthalazine
keywords: Anticancer; Apoptosis; Cell cycle arrest; Phthalazine; Triazole