1016752-48-9Relevant academic research and scientific papers
Amide derivatives of Gallic acid: Design, synthesis and evaluation of inhibitory activities against in vitro α-synuclein aggregation
Bai, Su-Ping,Chen, Li,Huang, Guo-Long,Lü, Ming-Huan,Xu, Ji,Zhang, Yun-Xiao
, (2020)
Gallic acid (GA), a natural phenolic acid, has received numerous attention because of its anti-oxidative, anti-inflammatory, and anti-cancer activity. More importantly, GA can act as an efficient inhibitor of α-Synuclein (α-Syn) aggregation at early stages. Nevertheless, some evidences suggest that GA is unlikely to cross the blood–brain barrier because of its high hydrophilicity. Hence, GA may not be considered as a promising candidate or entering brain and directly affecting the central nervous system. Accordingly, we have designed and synthesized a series of amide derivatives of GA, some of which possess appropriate lipophilicity and hydrophilicity with LogP (2.09–2.79). Meanwhile, these sheet-like conjugated compounds have good π-electron delocalization and high ability of hydrogen-bond formation. Some compounds have shown better in vitro anti-aggregation activities than GA towards α-Syn, with IC50 down to 0.98 μM. The valid modification strategy of GA is considered an efficient way to discover novel inhibitors of α-Syn aggregation.
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors
Karra, Srinivasa,Xiao, Yufang,Chen, Xiaoling,Liu-Bujalski, Lesley,Huck, Bayard,Sutton, Amanda,Goutopoulos, Andreas,Askew, Ben,Josephson, Kristopher,Jiang, Xuliang,Shutes, Adam,Shankar, Vikram,Noonan, Tom,Garcia-Berrios, Gaianne,Dong, Rong,Dhanabal, Mohanraj,Tian, Hui,Wang, Zhenxiong,Clark,Goodstal, Samantha
, p. 3081 - 3087 (2013/06/26)
Several potent Aurora kinase inhibitors derived from 5H-benzo[c][1,8] naphthyridin-6-one scaffold were identified. A crystal structure of Aurora kinase A in complex with an initial hit revealed a binding mode of the inhibitor within the ATP binding site and provided insight for structure-guided compound optimization. Subsequent SAR campaign provided a potent and selective pan Aurora inhibitor, which demonstrated potent target modulation and antiproliferative effects in the pancreatic cell line, MIAPaCa-2. Furthermore, this compound inhibited phosphorylation of histone H3 (pHH3) in mouse bone morrow upon oral administration, which is consistent with inhibition of Aurora kinase B activity.
NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS
-
Page/Page column 46-47, (2010/04/03)
Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative di
