234751-02-1Relevant articles and documents
Theoretical and experimental design of atypical kinase inhibitors: Application to p38 MAP kinase
McClure, Kim F.,Abramov, Yuriy A.,Laird, Ellen R.,Barberia, John T.,Cai, Weiling,Carty, Thomas J.,Cortina, Santo R.,Danley, Dennis E.,Dipesa, Alan J.,Donahue, Kathleen M.,Dombroski, Mark A.,Elliott, Nancy C.,Gabel, Christopher A.,Han, Seungil,Hynes, Thomas R.,LeMotte, Peter K.,Mansour, Mahmoud N.,Marr, Eric S.,Letavic, Michael A.,Pandit, Jayvardhan,Ripin, David B.,Sweeney, Francis J.,Tan, Douglas,Tao, Yong
, p. 5728 - 5737 (2005)
Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described. A set of calculated descriptors relevant to the anticipated binding interaction for the fragments 1-methyl-
Synthesis and applications of novel aminopyrazole derivative
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, (2020/04/17)
The invention discloses a novel kinase inhibitor aminopyrazole derivative, a preparation method and medical applications thereof, and more specifically relates to an aminopyrazole derivative containing benzimidazole, and a preparation method thereof, wher
Design, synthesis and biological evaluation: 5-amino-1h-pyrazole-1-carbonyl derivatives as fgfr inhibitors
Zhang, Yan,Yu, Niefang
, p. 1330 - 1341 (2020/10/06)
Background: Fibroblast growth factors (FGFs) and their high affinity receptors (FGFRs) play a major role in cell proliferation, differentiation, migration, and apoptosis. Aberrant FGFR signaling pathway might accelerate development in a broad panel of mal
Oxygen-containing five-membered heterocyclic compound, synthesis method, pharmaceutical composition and application
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Paragraph 0125; 0145-0147; 0175; 0188-0190, (2020/11/10)
The invention discloses an oxygen-containing five-membered heterocyclic compound, a synthesis method, a pharmaceutical composition and application thereof, and belongs to the technical field of medicines and preparation and application thereof. The oxygen-containing five-membered heterocycle has the biological activity of inhibiting the protein tyrosine phosphatase SHP2, can be used as a tool compound for researching the biological function relevance of the protein tyrosine phosphatase SHP2 in the cell signal transduction process, and provides a new means for preventing and treating cancers and metabolic and immune diseases.
Synthesis of Aminofuran-Linked Benzimidazoles and Cyanopyrrole-Fused Benzimidazoles by Condition-Based Skeletal Divergence
Hsu, Wei-Shun,Tsai, Min-Huan,Barve, Indrajeet J.,Yellol, Gorakh S.,Sun, Chung-Ming
, p. 492 - 499 (2017/07/15)
A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, w
Diversity-Oriented Synthesis of Coumarin-Linked Benzimidazoles via a One-Pot, Three-Step, Intramolecular Knoevenagel Cyclization
Yao, Po-Hsin Eric,Kumar, Sunil,Liu, Yu-Li,Fang, Chiu-Ping,Liu, Chia-Chen,Sun, Chung-Ming
supporting information, p. 271 - 275 (2017/04/21)
Diversity-oriented synthesis of coumarin-linked benzimidazoles from N-(2-aminophenyl)-2-cyanoacetamide was achieved via a one-pot, three-step sequential reaction in excellent yields. In situ intramolecular cyclization of the cyanoacetamide afforded benzimidazoles which subsequently underwent a Knoevenagel condensation of the 2-cyanomethylbenzimidazoles with salicylaldehydes promoted by triethylamine to reach the target compounds. An important intermediate, 2-(2-imino-2H-chromen-3-yl)-1H-benzimidazole was characterized by X-ray analysis and further hydrolyzed to 2-(coumarin-3-yl)benzimidazole in acidic condition. Among the synthesized compounds, some were found to be promising inhibitors of porcine kidney d-amino acid oxidase (pkDAO).
Copper catalyzed aerobic oxidative cyclization and ketonization: One pot synthesis of benzoimidazo[1,2-: A] imidazolones
Selvaraju, Manikandan,Ye, Tzuen-Yang,Li, Chia-Hsin,Ho, Pei-Heng,Sun, Chung-Ming
supporting information, p. 6621 - 6624 (2016/06/01)
A highly efficient synthesis of benzoimidazo[1,2-a]imidazolone through a novel oxidative 5-exo-dig cyclization-ketonization cascade of 2-aminobenzimidazole, aldehyde and terminal alkyne has been explored under aerobic conditions. The reaction proceeds thr
Three Component Divergent Reactions: Base-Controlled Amphiphilic Synthesis of Benzimidazole-Linked Thiazetidines and Fused Thiadiazines
Selvaraju, Manikandan,Dhole, Sandip,Sun, Chung-Ming
, p. 8867 - 8875 (2016/10/14)
A divergent reaction of 2-aminobenzimidazole with isothiocyanates and dihalomethanes has been developed for the selective synthesis of benzoimidazothiazetidine and benzoimidazothiadiazine. A single-pot reaction of 2-aminobenzimidazole in the presence of s
Synthesis and bioevaluation of pyrazole-benzimidazolone hybrids as novel human 4-Hydroxyphenylpyruvate dioxygenase inhibitors
Xu, Yu-Ling,Lin, Hong-Yan,Ruan, Xu,Yang, Sheng-Gang,Hao, Ge-Fei,Yang, Wen-Chao,Yang, Guang-Fu
, p. 427 - 438 (2015/03/05)
4-Hydroxyphenylpyruvate dioxygenase (HPPD), an essential enzyme in tyrosine catabolism, is an important target for treating type I tyrosinemia. Inhibition of HPPD can effectively alleviate the symptoms of type I tyrosinemia. However, only one commercial H
A concise synthesis of 2-(2-aminothiophene)-benzimidazoles by one-pot multicomponent reaction
Chen, Li-Hsun,Chuang, Ying-Sheng,Narhe, Bharat D.,Sun, Chung-Ming
, p. 13934 - 13943 (2013/08/23)
A one-pot synthesis of 2-aminothiophene linked benzimidazoles was achieved by utilizing 2-cyanomethyl benzimidazoles in a modified Gewald multicomponent reaction. The synthetic strategy of the reaction involved treatment of 2-(cyanomethyl)-benzimdazole wi