76006-04-7Relevant academic research and scientific papers
ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 1134, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
Novel pyrazolopyridine derivatives as potential angiogenesis inhibitors: Synthesis, biological evaluation and transcriptome-based mechanistic analysis
Michailidou, Maria,Giannouli, Vassiliki,Kotsikoris, Vasilios,Papadodima, Olga,Kontogianni, Georgia,Kostakis, Ioannis K.,Lougiakis, Nikolaos,Chatziioannou, Aristotelis,Kolisis, Fragiskos N.,Marakos, Panagiotis,Pouli, Nicole,Loutrari, Heleni
, p. 143 - 157 (2016/06/09)
Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed and synthesized a new series of substituted pyrazolopyridines and explored their ability to influence crucial pro-angiogenic attributes of endothelial cells. Four of the synthesized compounds, possessing analogous substitution pattern, were found able to inhibit at low micromolar concentrations endothelial cell proliferation, migration and differentiation, constitutively or in response to Vascular Endothelial Growth Factor (VEGF) and to attenuate VEGF-induced phosphorylation of VEGF receptor-2 and downstream kinases AKT and ERK1/2. Administration of effective compounds in mice delayed the growth of syngeneic Lewis lung carcinoma transplants and reduced tumor microvessel density, without causing toxicity. Genome-wide microarray and gene ontology analyses of treated endothelial cells revealed derivative 18c as the most efficient modulator of gene expression and mitotic cell cycle/cell divisiong along with ? cholesterol biosynthesis? as the most significantly altered biological processes.
Synthesis of two 'heteroaromatic rings of the future' for applications in medicinal chemistry
Silva Júnior,Rezende,Gimenes, Julia Possamai,Maltarollo, Vinícius Gonc?lves,Dale, James,Trossini,Emery,Ganesan
, p. 22777 - 22780 (2016/03/26)
In a computational study, the 1H-pyrazolo[3,4-c]pyridin-5-ol and 2,6-naphthyridin-3-ol heterocycles were identified as unknown heteroaromatic ring systems of potential value for medicinal chemistry. Here we report robust and concise synthetic protocols that provide access to these two scaffolds on a multigram scale.
Pyrazolopyridines. Part 5. Preparation and Reactions of Pyrazolopyridines
Chapman, David,Hurst, Jim
, p. 2398 - 2404 (2007/10/02)
A series of pyrazolopyridines has been prepared by nitrosation of 3-acetamido-4-methylpyridines and subsequent rearrangement and cyclisation of the N-acetyl-N-nitroso-compounds produced.The reactions of the pyrazolopyridines have been investigated. 1- and 2-Acetyl and 1- and 2-benzyl compounds were obtained and their structures elucidated spectroscopically.The ring system readily undergoes electrophilic substitution in the 3-position. 7-Chloropyrazolopyridine has been shown to be more susceptible to nucleophilic substitution than the isomeric 5-chloro-compound.
