《Synthesis and in vitro and in vivo biological evaluation of novel derivatives of flexicaulin A as antiproliferative agents》 was written by Huo, Jun-Feng; Hu, Tian-Xing; Dong, Ya-Long; Zhao, Jin-Zhu; Liu, Xiao-Jie; Li, Lei-Lei; Zhang, Xue-Yan; Li, Yun-Fan; Liu, Hong-Min; Ke, Yu; Wang, Cong. SDS of cas: 2623-87-2 And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
As our research focuses on anticancer drugs, a series of novel derivatives of flexicaulin A (I), an ent-kaurene diterpene, condensed with an aromatic ring were synthesized, and their antiproliferative activities against four human cancer cell lines (TE-1, EC109, MCF-7, and MGC-803) were evaluated. The activities of most of the new compounds were better than those of I. Compound II exhibited the best activity with an IC50 value reaching 0.13μM against oesophageal cancer cells (EC109 cells). The IC50 values for II in normal cells (GES-1 cells and HUVECs) were 0.52μM and 0.49μM, resp. Subsequent mechanistic investigations found that compound II can inhibit the proliferation of cancer cells and cell cloning. In addition, II could reduce the mitochondrial membrane potential, increase the apoptosis rate, and increase the ROS level in EC109 cells. Moreover, II can upregulate the expression of ROS/JNK pathway-related proteins (p-ASK1, p-MKK4, p-JNK, and p-Cjun (ser63)) and pro-apoptotic proteins (Bax, Bad, and Bim). In vivo experiments showed that II can inhibit tumor growth in nude mice. The mechanism involves an increase in protein expression in the ROS pathway, leading to changes in apoptosis-related proteins. In addition, compound II shows low toxicity. These results indicate that compound II holds promising potential as an antiproliferative agent. In the part of experimental materials, we found many familiar compounds, such as 4-Bromobutanoic acid(cas: 2623-87-2SDS of cas: 2623-87-2)
4-Bromobutanoic acid(cas: 2623-87-2) belongs to carboxylic acids. The chief chemical characteristic of the carboxylic acids is their acidity. They are generally more acidic than other organic compounds containing hydroxyl groups but are generally weaker than the familiar mineral acids (e.g., hydrochloric acid, HCl, sulfuric acid, H2SO4, etc.).SDS of cas: 2623-87-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary