3380-62-9Relevant academic research and scientific papers
Design and synthesis of β-carboline and combretastatin derivatives as anti-neutrophilic inflammatory agents
Kumar, Sunil,Wang, Yi-Hsuan,Chen, Po-Jen,Chang, Yu-Chia,Kashyap, Hemant K.,Shen, Ya-Ching,Yu, Huang-Ping,Hwang, Tsong-Long
, (2021/04/09)
A series of β-carboline derivatives was synthesized by the Pictet-Spengler reaction with or without the combretastatin skeleton. The structures of these derivatives were elucidated by spectroscopic techniques. All synthesized compounds were evaluated for
Tetrahydro Beta-carboline derivative as well as preparation method and application of derivative
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Paragraph 0060; 0161, (2018/04/26)
The invention discloses a tetrahydro Beta-carboline derivative shown in a formula I as described in the specification, which is a novel compound with histone deacetylase inhibiting activity and can beused for treating some diseases with abnormally high expression of histone deacetylase effectively. The histone deacetylase is closely related to occurrence and development of cancers. The serial compounds can inhibit proliferation of tumor cells effectively by inhibiting the activity of the histone deacetylase and inducing differentiation and apoptosis of the tumor cells, so as to achieve the purpose of treating cancers.
Mild and efficient cyanuric chloride catalyzed Pictet-Spengler reaction
Sharma, Ashish,Singh, Mrityunjay,Rai, Nitya Nand,Sawant, Devesh
, p. 1235 - 1242 (2013/07/26)
A practical, mild and efficient protocol for the Pictet-Spengler reaction catalyzed by cyanuric chloride (trichloro-1,3,5-triazine, TCT) is described. The 6-endo cyclization of tryptophan/tryptamine and modified Pictet-Spengler substrates with both electr
Water as an efficient medium for the synthesis of tetrahydro-β-carbolines via Pictet-Spengler reactions
Saha, Biswajit,Sharma, Sunil,Sawant, Devesh,Kundu, Bijoy
, p. 1379 - 1383 (2007/10/03)
A mild and efficient protocol for the Pictet-Spengler reaction in water using an acid catalyst has been described. The condensation of tryptophan, tryptamine, and Nb-benzyl tryptophan with different aldehydes having both electron-withdrawing and -donating substituents in the presence of a catalytic amount of TFA in water furnished tetrahydro-β-carbolines in good isolated yields. A salient feature of the water mediated Pictet-Spengler reaction was the general trend observed during the condensation of Trp-OMe and aryl/aliphatic aldehydes furnishing diastereomeric mixtures with a preference for the cis-isomer.
The preparation and evaluation of 1-substituted 1,2,3,4-tetrahydro- and 3,4-dihydro-β-carboline derivatives as potential antitumor agents
Shen, Ya-Ching,Chen, Ching-Yeu,Hsieh, Pei-Wen,Duh, Chang-Yih,Lin, Yat-Min,Ko, Chin-Lien
, p. 32 - 36 (2007/10/03)
A series of 1-substituted 1,2,3,4-tetrahydro- and 3,4-dihydro-β- carboline derivatives have been synthesized and evaluated for antitumor activity against murine P-388 and human tumor cell lines, KB-16, A-549 and HT-29. All of the compounds prepared, excep
1-substituted 1,2,3,4-tetrahydro-beta-carboline and 3,4-dihydro-beta-carboline and analogs as antitumor agents
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, (2008/06/13)
A composition includes a substituted dihydro- or tetrahydro-β-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-β-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.
Mild Oxidation of 1,2,3,4-Tetrahydro-β-carbolines
Mokrosz, M.J.,Paluchowska, M.H.,Misztal, S.
, p. 264 - 268 (2007/10/02)
Oxidation of 1-(aryl or heteroaryl)-1,2,3,4-tetrahydro-β-carbolines (1a-r) with KMnO4 in dry THF afforded in the most cases almost exclusively 3,4-dihydro products (2) with a yield of 28-94percent.Only in few cases (1c, 1i, 1m) the reaction was non-selective and a significant amount of the fully aromatized products (3) (30-40percent of the reaction mixture) was observed.The influence of both the substituent nature and the substitution modes on the observed yield and selectivity of the reaction was discussed.Key words: 1,2,3,4-tetrahydro-β-carbolines, 3,4-dihydro-β-carbolines, selective oxidation, oxidation with KMnO4 in cold THF, substituent effect
