title: Synthesis and biological evaluation of novel steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines.
abstract: The preparation of steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines and their biological evaluation as potential anticancer agents are herein reported. These novel heterosteroids (2, 4) were prepared through the condensation reaction of 3-amino-1,2,4-triazole with 16-arylidene-17-ketosteroids (1, 3). All the synthesized compounds were evaluated for their anticancer activity in vitro against PC-3 (human prostatic carcinoma), MCF-7 (human breast carcinoma) and EC9706 (human esophageal carcinoma) cell lines. Among the screened compounds, 2i, 2n and 4f showed significant inhibitory activity against all the three human cell lines.
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Li-Hua
authors.initials: LH
authors.lastname: Huang
authors.forename: Yong-Fei
authors.initials: YF
authors.lastname: Zheng
authors.forename: Yong-Zheng
authors.initials: YZ
authors.lastname: Lu
authors.forename: Chuan-Jun
authors.initials: CJ
authors.lastname: Song
authors.forename: Yan-Guang
authors.initials: YG
authors.lastname: Wang
authors.forename: Bin
authors.initials: B
authors.lastname: Yu
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; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D006801:Humans; D020128:Inhibitory Concentration 50; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D013256:Steroids; D014230:Triazoles