84518-77-4Relevant academic research and scientific papers
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.
?-CARBOLINE, DIHYDRO-?-CARBOLINE AND TETRAHYDRO-?-CARBOLINE ALKALOID DERIVATIVES AND PREPARATION METHODS SAME AND USE IN ASPECTS OF PREVENTING AND TREATING PLANT VIRUSES, FUNGICIDES AND INSECTICIDES
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Paragraph 0165-0166, (2016/11/28)
The present invention relates to β-carboline, dihydro-β-carboline and tetrahydro-β-carboline alkaloid derivatives (I) and a method for preparing same and the use in the aspects of preventing and treating plant viruses, fungicides and insecticides. For the meaning of each group in formula (I) see the description. The β-carboline, dihydro-β-carboline and tetrahydro-β-carboline alkaloid derivatives of the present invention show a particularly ourstanding anti-plant virus activity, and also have fungicidal and insecticidal activities.
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 and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents
Sun, Rongqin,Liu, Rui,Zhou, Chi,Ren, Zhenghua,Guo, Liang,Ma, Qin,Fan, Wenxi,Qiu, Liqin,Yu, Huijuan,Shao, Guang,Cao, Rihui
, p. 2170 - 2174 (2015/12/11)
A series of novel bivalent β-carbolines with a piperazine group spacer between 3-methylene units were synthesized and evaluated as antitumor agents. The results demonstrated that compounds 7e and 7g exhibited the most potent cytotoxic activities against ten tumor cell lines. Structure-activity relationships analysis indicated that (1) the substituents in positions 1 and 9 of the β-carboline ring played a significant role in modulating the antitumor activity; (2) the introduction of alkyl groups into position-9 of the β-carboline nucleus enhanced their cytotoxic potencies and the butyl substituent was the optimal group. Investigation of the preliminary mechanism of action demonstrated that compound 7g showed obvious anti-angiogenic activity in the in vivo CAM assay, and the potency was similar to that of CA4P (200 μM).
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.
Synthesis and structure of the β-carboline derivatives and their binding intensity with cyclin-dependent kinase 2
Wang, Yue,Jin, Qiaomei,Lin, Guowu,Yang, Taotao,Wang, Zhanwei,Lu, Yi,Tang, Yimin,Liu, Lifang,Lu, Tao
, p. 435 - 441 (2012/05/04)
Series of 3-substituted of 6-aminosulfonyl-β-carbolines were designed and synthesized. In addition, the binding mode of these β-carboline derivatives with cyclin-dependent kinase 2 (CDK2) was studied by means of fluorescence measurements and molecular doc
Synthesis of a novel series of 1,6-disubstituted-3-(cyclohexylmethoxy)- β-carboline derivatives via Minisci reaction
Lin, Guowu,Wang, Yue,Zhou, Qingfa,Wang, Jian,Yang, Taotao,Wang, Zhanwei,Lu, Tao
, p. 1895 - 1910 (2012/06/18)
A facile and efficient route for the synthesis of 1,6-disubstituted-3- cyclohexylmethoxy-β-carboline derivatives via the Minisci reaction has been described with good yields and selectivity. A novel series of β-carboline derivatives with various substitue
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse
Yin, Wenyuan,Majumder, Samarpan,Clayton, Terry,Petrou, Steven,Vanlinn, Michael L.,Namjoshi, Ojas A.,Ma, Chunrong,Cromer, Brett A.,Roth, Bryan L.,Platt, Donna M.,Cook, James M.
experimental part, p. 7548 - 7564 (2011/01/04)
A series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at αxβ 3γ2 GABAA/benzodiazepine receptor subtypes by radioligand binding assays in search of α1 s
A facile synthesis of 3-substituted 9H-pyrido[3,4-b]indol- 1(2H)-one derivatives from 3-substituted β-carbolines
Lin, Guowu,Wang, Yue,Zhou, Qingfa,Tang, Weifang,Wang, Jian,Lu, Tao
scheme or table, p. 5680 - 5691 (2010/12/19)
A mild and efficient two-step synthesis of 3-substituted β-carbolinone derivatives from 3-substituted β-carboline in good yields is described. A possible reaction mechanism for the formation of the skeleton of β-carbolin-1-one is proposed. The structures of these compounds were established by IR, 1H-NMR, 13C-NMR, mass spectrometry and elemental analysis, as well as X-ray crystallographic analysis of 4-2 and 6-2.
OXADIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Page/Page column 56, (2009/07/17)
Oxadiazole derivatives of formula (I) where ring A is a bicyclic or tricyclic system. Claimed compounds are active on nicotinic acetylcholine receptors (nAChRs), and are useful to treat neurological, psychiatric, and gastrointestinal disorders, as well as sepsis and obesity.
