105105-00-8Relevant articles and documents
Convenient synthesis of 7-hydroxyindole
Ishiyama, Kazunao,Yamada, Yasuhiro
, p. 1021 - 1022 (2005)
7-Hydroxyindole, the key building block for the synthesis of AJ-9677 1, was prepared from indoline in six steps in 36% overall yield. AJ-9677 1 is a potent and selective adrenaline β3-agonist being considered as a clinical candidate to treat obesity in those who are suffering from diabetes.
Structural Insights into Notum Covalent Inhibition
Zhao, Yuguang,Svensson, Fredrik,Steadman, David,Frew, Sarah,Monaghan, Amy,Bictash, Magda,Moreira, Tiago,Chalk, Rod,Lu, Weixian,Fish, Paul V.,Jones, E. Yvonne
, p. 11354 - 11363 (2021/08/16)
The carboxylesterase Notum hydrolyzes a palmitoleate moiety from Wingless/Integrated(Wnt) ligands and deactivates Wnt signaling. Notum inhibitors can restore Wnt signaling which may be of therapeutic benefit for pathologies such as osteoporosis and Alzhei
Lactam derivative as well as preparation method and medical application thereof
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Paragraph 0116-0126, (2020/12/30)
The invention relates to lactam derivatives, and a preparation method and medical application thereof. Specifically, the invention relates to lactam derivatives as shown in a general formula (I), a preparation method of the lactam derivatives, pharmaceuti
INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD
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Page/Page column 46-47, (2010/04/03)
The subject invention concerns methods and compounds for inhibiting Shp2. In one embodiment, a compound of the invention has a chemical structure as shown in formula I or II: wherein X, Y, and Z are independently N or S; R1 is cycloalkyl, heter
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: A novel series of mixed dopamine D2/D4 receptor antagonist
Zhao, He,Zhang, Xiaoyan,Hodgetts, Kevin,Thurkauf, Andrew,Hammer, Jack,Chandrasekhar, Jayaraman,Kieltyka, Andrzej,Brodbeck, Robbin,Rachwal, Stanislaw,Primus, Renee,Manly, Charles
, p. 701 - 704 (2007/10/03)
5-Piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives were designed, synthesized, and identified as a new series of mixed dopamine D2/D4 receptor antagonists. This series featured a rigid tricyclic ring system
Rational Design of an Indolebutanoic Acid Derivative as a Novel Aldose Reductase Inhibitor Based on Docking and 3D QSAR Studies of Phenethylamine Derivatives
Sun, Won Suck,Park, Yoon Sun,Yoo, Jakyung,Park, Ki Duk,Kim, Sung Han,Kim, Jung-Han,Park, Hyun-Ju
, p. 5619 - 5627 (2007/10/03)
A series of 45 phenethylamine derivatives were synthesized and evaluated for their inhibitory activity against pig kidney aldose reductase (ALR2, EC 1.1.1.21). Their IC50 values ranged from 400 μM to 24 μM. The binding modes of compounds at the active site of ALR2 were examined using flexible docking. The results indicated that phenethylamine derivatives nicely fit into the active pocket of ALR2 by forming various hydrogen bonding and hydrophobic interactions. 3D-QSAR analysis was also conducted using FlexX-docked alignment of the compounds. The best prediction was obtained by CoMSIA combined with hydrophobic and hydrogen bond donor/acceptor field (q 2 = 0.557, r2 = 0.934). A new derivative, 4-oxo-4-(4-hydroxyindole)butanoic acid, was designed, taking into account the CoMSIA field and the binding mode derived by FlexX docking. This rationally designed compound exhibits an ALR2 inhibition with an IC50 value of 7.4 μM, which compares favorably to that of a well-known ALR2 inhibitor, tolrestat (IC50 = 16 μM) and represents a potency approximately 240-fold higher than that of an original phenethylamine lead compound, YUA001.