title: Preparation of a series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety and examination of their cytotoxicity.
abstract: The chalcone basic skeleton is a unique template which is associated with widespread biological activities. In the present study, a series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety was prepared through Mannich reaction and Clasien-Schmidt condensation. The synthetic analogs 2-16 were subjected into the cytotoxicity examinations using a panel of 25 human tumor cell lines. Among the tested compounds, 3 and 4 which possessed the 3-pyridyl and phenyl groups as the substructure, respectively, displayed significant cytotoxicity against all the tumor cell lines. The results suggested that these bichalcones were potential to be the anticancer lead drugs.
authors: Department of Chemistry, National Cheng Kung University, Tainan 70101, Taiwan, ROC.
authors: Mopuru Vijaya Bhaskar
authors: MV
authors: Reddy
authors: Shih-Shun
authors: SS
authors: Chen
authors: Meng-Liang
authors: ML
authors: Lin
authors: Hsiu-Hui
authors: HH
authors: Chan
authors: Ping-Chung
authors: PC
authors: Kuo
authors: Tian-Shung
authors: TS
authors: Wu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010879:Piperazines; D002599:Chalcone