4036-83-3Relevant articles and documents
Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects
Cao, Zhi,Guo, Ming,Jiang, Nan,Li, Changtao,Li, Tong,Wang, Xinyu,Yang, Jing,Zhai, Xin
, (2021/10/06)
In order to explore novel TRK and ALK dual inhibitors, a series of 2-phenylamino-4-prolylpyrimidine derivatives were designed, synthesized and evaluated for their in vitro cytotoxicity and enzymatic activities. Delightfully, most compounds were detected m
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2
Tian, Wei,Guo, Jiapeng,Zhang, Qingsen,Fang, Shaoyu,Zhou, Ruolan,Hu, Jian,Wang, Mingping,Zhang, Yuefan,Guo, Jin-Min,Chen, Zhuo,Zhu, Ju,Zheng, Canhui
, (2020/12/30)
Aldehyde dehydrogenase 2 (ALDH2) plays important role in ethanol metabolism, and also serves as an important shield from the damage occurring under oxidative stress. A special inactive variant was found carried by 35–45% of East Asians. The variant carriers have recently been found at the higher risk for the diseases related to the damage occurring under oxidative stress, such as cardiovascular and cerebrovascular diseases. As a result, ALDH2 activators may potentially serve as a new class of therapeutics. Herein, N-benzylanilines were found as novel allosteric activators of ALDH2 by computational virtual screening using ligand-based and structure-based screening parallel screening strategy. Then a structural optimization was performed and has led to the discovery of the compound C6. It has good activity in vitro and in vivo, which could reduce infarct size by ~70% in ischemic stroke rat models. This study provided good lead compounds for the further development of ALDH2 activators.
ALDH2 agonist, preparation method and application thereof
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Paragraph 0135-0137; 0139-0140, (2019/07/10)
The invention belongs to the technical field of medicines, and particularly relates to an ALDH2 agonist, a preparation method and application thereof. The ALDH2 agonist has a novel structure and excellent ALDH2 agonist activity.