A mild and concise [3+2] coupling of quinonemonoacetals or quinoneimineketals with vinylcarbamates promoted by Lewisacid was realized. Various 2-carbamate-2,3-dihydrobenzofurans and 2-carbamate-indolines have been prepared in moderate to good yields.
[EN] SYNTHESIS OF MONOCYCLIC N-PYRIDYL-1, 4-AZABORINES AND THEIR PT-COORDINATION COMPLEXES<br/>[FR] SYNTHÈSE DE N-PYRIDYL-1,4-AZABORINES MONOCYCLIQUES ET LEURS COMPLEXES DE COORDINATION PT
申请人:OREGON STATE
公开号:WO2015126400A1
公开(公告)日:2015-08-27
Monocyclic N-pyridyl-1,4-azaborines and their Pt coordination complexes.
单环N-吡啶基-1,4-氮硼杂环烷及其铂配合物。
A Boronic Acid Conjugate of Angiogenin that Shows ROS-Responsive Neuroprotective Activity
作者:Trish T. Hoang、Thomas P. Smith、Ronald T. Raines
DOI:10.1002/anie.201611446
日期:2017.3.1
hemorrhage and encourage tumor growth. The causal neurodegeneration of ALS is associated with reactive oxygen species, which are also known to elicit the oxidative cleavage of carbon–boronbonds. We have developed a synthetic boronic acid mask that restrains the ribonucleolytic activity of ANG. The masked ANG does not stimulate endothelial cell proliferation but protects astrocytes from oxidative stress
血管生成素 (ANG) 是一种人类核糖核酸酶,在肌萎缩侧索硬化症 (ALS) 患者中会受到损害。ANG还促进新血管形成,并可诱发出血并促进肿瘤生长。ALS 的因果神经变性与活性氧有关,活性氧也会引起碳硼键的氧化断裂。我们开发了一种合成硼酸面膜,可以抑制 ANG 的核糖核酸分解活性。掩蔽的 ANG 不会刺激内皮细胞增殖,但会保护星形胶质细胞免受氧化应激。通过区分 ANG 的两种二分生物活性,该策略可以为 ALS 的治疗提供可行的药理学方法。
[EN] ANGIOGENIN-BORONIC ACID CONJUGATES WITH SELECTIVE NEUROPROTECTION ACTIVITY<br/>[FR] CONJUGUÉS ANGIOGÉNINE-ACIDE BORIQUE AYANT UNE ACTIVITÉ DE NEUROPROTECTION SÉLECTIVE
申请人:WISCONSIN ALUMNI RES FOUND
公开号:WO2018119432A1
公开(公告)日:2018-06-28
Masked h-ANG variant conjugates useful for protection of cells, particularly neuronal cells from injury and death, particularly from injury and death associated with ROS (reactive oxygen species). Masked h-Ang variant conjugates do not exhibit ribonucleolytic activity until unmasked. Masked h-ANG variant conjugates are activatable by reaction with ROS and exhibit ribonucleolytic activity only after reaction with ROS. Masked h-ANG variant conjugates are useful in the treatment of neurodegenerative diseases and disorders, such as amyotrophic lateral sclerosis. Certain h-ANG variants in which lysine at position 40 is replaced with cysteine are provided at least as starting materials for making masked h-ANG variant conjugates. Certain h-ANG variants in which lysine at position 40 is replaced with thialysine are generated on unmasking of h-ANG variant conjugates and exhibit ribonucleolyitc activity.
The invention of radical reactions. Part XXXIV. Homologation of carboxylic acids to α-keto carboxylic acids by Barton-ester based radical chain chemistry
Carboxylicacids can be transformed into the homologous α-ketoacids by Barton-esterbasedradicalchemistry. This method was especially successful when ethyl α-trifluoroacetoxy acrylate was used as a radical trap.