Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors was written by Yu, Zhiliang;Zhuang, Chunlin;Wu, Yuelin;Guo, Zizhao;Li, Jin;Dong, Guoqiang;Yao, Jianzhong;Sheng, Chunquan;Miao, Zhenyuan;Zhang, Wannian. And the article was included in International Journal of Molecular Sciences in 2014.COA of Formula: C7H5ClF2 This article mentions the following:
A series of sulfamide I (R1 = HCCCH2, 3-FC6H4CH2, NCCH2, 2,6-F2C6H3CH2, C6H5CH2; R2 = HCCCH2, H2C:C:CH, H) and triazole benzodiazepines, e.g. II, were obtained with the principle of bioisosterism. The p53-murine double minute 2 (MDM2) inhibitory activity and in vitro antitumor activity were evaluated. Most of the benzodiazepines exhibited moderate protein binding inhibitory activity. The triazole benzodiazepines showed good inhibitory activity and antitumor potency. The compound 8-chloro-4-(4-chloro-phenyl)-6-phenyl-4H-2,3,5,10b-tetraaza-benzo[e]azulene had promising antitumor activity against the U-2 OS human osteosarcoma cell line with an IC50 value of 4.17 μM, which was much better than that of nutlin-3. The mol. docking model also successfully predicted that this class of compounds mimicked the three critical residues of p53 binding to MDM2. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4COA of Formula: C7H5ClF2).
2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.COA of Formula: C7H5ClF2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics