Design, synthesis and biological evaluation of novel pyrrolidone-based derivatives as potent p53-MDM2 inhibitors was written by Si, Dongjuan;Luo, Huijuan;Zhang, Xiaomeng;Yang, Kundi;Wen, Hongmei;Li, Wei;Liu, Jian. And the article was included in Bioorganic Chemistry in 2021.Application In Synthesis of 2,5-Difluorophenylacetyl chloride This article mentions the following:
Inhibition of the interactions of the tumor suppressor protein p53 with its neg. regulators MDM2 in vitro and in vivo, representing a valuable therapeutic strategy for cancer treatment. The natural product chalcone exhibited moderate inhibitory activity against MDM2, thus based on the binding mode between chalcone and MDM2, a hit unsaturated pyrrolidone scaffold was obtained through virtual screening. Several unsaturated pyrrolidone derivatives were synthesized and biol. evaluated. As a result, because the three critical hydrophobic pockets of MDM2 were occupied by the substituted-Ph linked at the pyrrolidone fragment, compound I demonstrated good binding affinity with the MDM2. Addnl., compound I also showed excellent antitumor activity and selectivity, and no cytotoxicity against normal cells in vitro. The further antitumor mechanism studies were indicated that compound I could successfully induce the activation of p53 and corresponding downstream p21 proteins, thus successfully causing HCT116 cell cycle arrest in the G1/M phase and apoptosis. Thus, the novel unsaturated pyrrolidone p53-MDM2 inhibitors could be developed as novel antitumor agents. In the experiment, the researchers used many compounds, for example, 2,5-Difluorophenylacetyl chloride (cas: 157033-23-3Application In Synthesis of 2,5-Difluorophenylacetyl chloride).
2,5-Difluorophenylacetyl chloride (cas: 157033-23-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Application In Synthesis of 2,5-Difluorophenylacetyl chloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics