84518-77-4Relevant articles and documents
Pd/C-Catalyzed Dehydrogenative [3+2] Cycloaddition for the Synthesis of Functionalized Tropanes
Wang, Hai-Jun,Guo, Lei,Zhu, Cheng-Feng,Luo, Yun-Fei,Li, You-Gui,Wu, Xiang
supporting information, p. 5456 - 5459 (2018/10/20)
A Pd/C-catalyzed cascade approach for the synthesis of attractive benzo-fused tropanes was developed. The reaction proceeds through a sequential Pd/C-catalyzed dehydrogenative formation of azomethine ylides from amines and 1,3-dipolar cycloaddition. It allows the generation of structurally complex benzo-fused tropanes in good yields with excellent diastereoselectivities under mild reaction conditions. Preliminary results of asymmetric version of the reaction reveal that the copper catalyst and chiral monophosphoramidite ligand can furnish optically active products with moderate ee.
Synthesis and biological evaluation of novel 3,9-substituted β-carboline derivatives as anticancer agents
Chen, Yi-Fong,Lin, Yi-Chien,Chen, Jeng-Pang,Chan, Hsu-Chin,Hsu, Mei-Hua,Lin, Hui-Yi,Kuo, Sheng-Chu,Huang, Li-Jiau
, p. 3873 - 3877 (2015/08/24)
Abstract In our previous studies on 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) analogs, we synthesised numerous substituted carbazole and α-carboline derivatives, which exhibited anticancer activity. In this study, we designed and synthesised a series of 3,9-substituted β-carbolines, by replacing the tricyclic rings of carbazole and α-carboline derivatives with isosteric β-carboline, and evaluated anticancer activity. We observed that 9-(2-methoxybenzyl)-β-carboline-3-carboxylic acid (11a) inhibited the growth of HL-60 cells by inducing apoptosis, with a half maximal inhibitory concentration of 4.0 μM. Our findings indicate that β-carboline derivatives can be used as lead compounds for developing novel antitumor agents.
Synthesis, characterization, DNA binding ability and cytotoxicity of the novel platinum(II), copper(II), cobalt(II) and nickel(II) complexes with 3-(1H-benzo[d]imidazol-2-yl)-β-carboline
Jin, Qiao-Mei,Lu, Yi,Jin, Jian-Lin,Guo, Hao,Lin, Guo-Wu,Wang, Yue,Lu, Tao
, p. 91 - 99 (2014/07/08)
3-(1H-benzo[d]imidazol-2-yl)-β-carbolin (Y-5) and its Pt(II), Cu(II), Co(II) and Ni(II) complexes 1-4 were synthesized and characterized by 1H NMR, MS, IR, elemental analyses and TG. Crystal structure of Y-5 and its Pt(II) complex were reported. The DNA binding and DNA cleavage ability of complexes with Cu(II) ion and Pt(II) ion as the metal center showed enhanced activities than that of the other two, which were evaluated by absorption spectra, EB displacement experiments and agarose gel electrophoresis. Assay on the cytotoxicity of the above complexes against A549 and Hela tumor cells and Helf normal cells revealed that the complexes 1 and 2 are toxic against tumor cells but relatively safe to normal cell.