Yan, Guoyi; Luo, Jiang; Han, Xuan; Zhang, Wenjuan; Pu, Chunlan; Zhou, Meng; Zhong, Xinxin; Hou, Xueyan; Hou, Man Zhou; Li, Rui published their research in Anti-Cancer Agents in Medicinal Chemistry in 2021. The article was titled 《Design, Synthesis and Biological Evaluation of 4, 6-Coumarin Derivatives as Anti- Cancer and Apoptosis-Inducing Agents》.Name: 2-(Piperidin-4-yl)ethanol The article contains the following contents:
Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents. The objective of the current work was the synthesis and biol. evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents. Thirty-seven coumarin derivatives were designed and synthesized, the antiproliferative activity of the compounds was evaluated against human cancer cell lines and non-cancerous cells by MTT assay. The bioactivities and underlying mechanisms of active mols. were studied and the ADMET characters were predicted. Among the compounds, 4-p-hydroxy phenol-6-pinacol borane coumarin (25) exhibited a promising anti-cancer activity to cancer cell lines in a dose-dependent manner and the toxicity to normal cells was low. The mechanism of action was observed by inducing G2/M phase arrest and apoptosis which was further confirmed via western blot. In silico ADMET prediction revealed that compound 25 is a drug-like small mol. with a favorable safety profile. The findings in this work may give vital information for further development of 6-pinacol borane coumarin derivatives as novel anti-cancer agents. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Name: 2-(Piperidin-4-yl)ethanol)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Name: 2-(Piperidin-4-yl)ethanol
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem