Discovery of novel tertiary amide derivatives as NEDDylation pathway activators to inhibit the tumor progression in vitro and in vivo was written by Fu, Dong-Jun;Song, Jian;Zhu, Ting;Pang, Xiao-Jing;Wang, Sheng-Hui;Zhang, Yan-Bing;Wu, Bo-Wen;Wang, Jun-Wei;Zi, Xiaolin;Zhang, Sai-Yang;Liu, Hong-Min. And the article was included in European Journal of Medicinal Chemistry in 2020.Computed Properties of C9H9ClO2 This article mentions the following:
NEDDylation pathway regulates multiple physiol. process, unlike inhibitors, NEDDylation activators are rarely studied. Novel amide derivatives were synthesized and evaluated for antiproliferative activity against MGC803, MCF-7 and PC-3 cells. Among them, VII-31 displayed the most potent activity with an IC50 value of 94 nmol/L against MGC803 cells. Cellular mechanisms elucidated that VII-31 inhibited the cell viability, arrested cell cycle at G2/M phase and induced apoptosis via intrinsic and extrinsic pathways against MGC803 cells. In addition, VII-31 activated NAE1-Ubc12-Cullin1 NEDDylation via interacting with NAE1 directly. Furthermore, the activation of NEDDylation resulted in the degradation of inhibitor of apoptosis proteins (IAPs). Importantly, VII-31 inhibited tumor growth in xenograft models in vivo without the apparent toxicity. In summary, it is the first time to reveal that VII-31 deserves consideration for cancer therapy as a NEDDylation activator. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Computed Properties of C9H9ClO2).
2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Computed Properties of C9H9ClO2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics