20776-45-8Relevant articles and documents
BIOMARKER PANEL TARGETED TO DISEASES DUE TO MULTIFACTORIAL ONTOLOGY OF GLYCOCALYX DISRUPTION
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, (2021/04/02)
The present disclosure provides biomarkers useful as companion diagnostics for detecting glycocalyx-based disease that is amenable to treatment using compounds designed for improving the condition of the glycocalyx and/or reducing inflammation and/or oxidative damage, as well as related compositions, kits, and methods.
Anti-tumor compounds
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Paragraph 0056; 0057; 0058; 0059; 0060, (2019/01/08)
The invention discloses anti-tumor compounds. The compounds target a Neddylation pathway. The compounds have a structural formula represented in a general formula I or a general formula II or a general formula III or a general formula IV or a general formula V or a general formula VI. The compounds have good anti-tumor activity, and multiple compounds are close to a positive control drug MLN4924,and can be used as good anti-tumor compounds. A combined therapy is provided through combined adoption of the compounds and compositions with other drugs, and a part of the same compositions can be formed by the drugs, or the drugs can be administered as separate components at the same time or at different time.
Asymmetric dearomatization of indoles through a Michael/Friedel-Crafts-Type cascade to construct polycyclic spiroindolines
Zhao, Xiaohu,Liu, Xiaohua,Mei, Hongjiang,Guo, Jing,Lin, Lili,Feng, Xiaoming
supporting information, p. 4032 - 4035 (2015/03/30)
A highly efficient asymmetric dearomatization of indoles was realized through a cascade reaction between 2-isocyanoethylindole and alkylidene malonates catalyzed by a chiral N,N-dioxide/MgII catalyst. Fused polycyclic indolines containing three stereocenters were afforded in good yields with excellent diastereo- and enantioselectivities through a Michael/Friedel-Crafts/Mannich cascade. When 2-substituted 2-isocyanoethylindoles were used, spiroindoline derivatives were obtained through a Michael/Friedel-Crafts reaction.
Synthesis and biological evaluation of novel tetrahydro-β-carboline derivatives as antitumor growth and metastasis agents through inhibiting the transforming growth factor-β signaling pathway
Zheng, Cong,Fang, Yuanzhang,Tong, Weiguang,Li, Guoliang,Wu, Haigang,Zhou, Wenbo,Lin, Qingxiang,Yang, Feifei,Yang, Zhengfeng,Wang, Peng,Peng, Yangrui,Pang, Xiufeng,Yi, Zhengfang,Luo, Jian,Liu, Mingyao,Chen, Yihua
, p. 600 - 612 (2014/03/21)
The transforming growth factor beta (TGFβ) signaling cascade is considered as one of the pivotal oncogenic pathways in most advanced cancers. Inhibition of the TGFβ signaling pathway by specific antagonists, neutralizing antibodies, or small molecules is considered as an effective strategy for the treatment of tumor growth and metastasis. Here we demonstrated the identification of a series of tetrahydro-β-carboline derivatives from virtual screening which potentially inhibit the TGFβ signaling pathway. Optimization of the initial hit compound 2-benzoyl-1,3,4,9-tetrahydro-β- carboline (8a) through substitution at different positions to define the structure-activity relationship resulted in the discovery of potent inhibitors of the TGFβ signaling pathway. Among them, compound 8d, one of the tested compounds, not only showed potent inhibition of lung cancer cell proliferation and migration in vitro but also strongly suppressed growth of lung cancer and breast cancer in vivo.
Antioxydant activity of β-carboline derivatives in the LDL oxidation model
Hadjaz, Fariza,Besret, Soizic,Martin-Nizard, Fran?oise,Yous, Sa?d,Dilly, Sébastien,Lebegue, Nicolas,Chavatte, Philippe,Duriez, Patrick,Berthelot, Pascal,Carato, Pascal
experimental part, p. 2575 - 2585 (2011/06/23)
A series of β-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO 4 or 2,2′-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R = 1.6 for 5 μM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R = 1.9 to 2.8 for 1 μM CuSO4. These substances have protective actions and increase significantly the cell viability.
A versatile linkage strategy for solid-phase synthesis of N,N-dimethyltryptamines and β-carbolines
Wu, Tom Y. H.,Schulte, Peter G.
, p. 4033 - 4035 (2007/10/03)
(matrix presented) Various tryptamines are captured by a vinylsulfonylmethyl polystyrene resin, generating a safety-catch linkage. β-Carbolines can be formed from 4 by a Pictet-Spengler reaction with the introduction of R1. Tryptamine 4 can also be derivatized by acylation or copper-mediated coupling to introduce R2. If X = Br, Suzuki coupling can be used to introduce R3. After derivatization, the indole derivatives are activated with methyl iodide and released under mild basic condition.
The chemistry of indoles. CIII. Simple syntheses of serotonin, N-methylserotonin, bufotenine, 5-methoxy-N-methyltryptamine, bufobutanoic acid, N-(indol-3-yl)methyl-5-methoxy-N-methyltryptamine, and lespedamine based on 1-hydroxyindole chemistry
Somei,Yamada,Kurauchi,Nagahama,Hasegawa,Yamada,Teranishi,Sato,Kaneko
, p. 87 - 96 (2007/10/03)
Application of regioselective nucleophilic substitution reactions of 1-hydroxytryptamines to novel and simple syntheses of serotonin (1a), N-methylserotonin (1b), bufotenine (1c), 5-methoxy-N-methyltryptamine (2a), bufobutanoic acid (3a), N-(indol-3-yl)methyl-5-methoxy-N-methyltryptamine (4), and lespedamine (5) are described. Effective syntheses of 5-benzyloxytryptamine and 1-methoxy-2-oxindoles are also reported.
The first total synthesis of bufobutanoic acid by two routes based on nucleophilic substitution reaction on indole nucleus
Kurauchi, Takashi,Nagahama, Yoshiyuki,Hasegawa, Masakazu,Yamada, Koji,Somei, Masanori
, p. 1017 - 1019 (2007/10/03)
Regioselective nucleophilic substitution reaction of 1- hydroxytryptamines led to establish two novel routes for the first synthesis of bufobutanoic acid. An effective synthesis of 5-benzyloxytryptamine from tryptamine is also reported.
