Facile synthesis of C1-substituted β-carbolines as CDK4 inhibitors for the treatment of cancer was written by Li, Deping;Liu, Wenwu;Huang, Yaoguan;Liu, Mingyue;Tian, Caizhi;Lu, Hongyuan;Jia, Hui;Xu, Zihua;Ding, Huaiwei;Zhao, Qingchun. And the article was included in Bioorganic Chemistry in 2022.Quality Control of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate This article mentions the following:
Cyclin-dependent kinase 4 (CDK4), which is involved in dynamic regulation of cell cycle, has gained particularly attention for its role in controlling tumor growth. Increasing evidence showed that β-carboline derivatives have the potential to inhibit CDK4. Herein, on the basis of previous work, authors designed and synthesized a series of novel β-carbolines and evaluated their antitumor activity. Among them, compounds I and II, with the most potent anti-proliferative activity and CDK4 enzymic inhibition activity, were selected for further pharmacol. research in vitro and in vivo. The results in vitro showed that I and II exhibited potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. In vivo, I showed significant tumor growth inhibition in HCT116 tumor xenograft model without causing significant weight loss and toxicity consistent with the acute toxicity test. In addition, silico study showed I and II not only have good biol. actions, but also acceptable predicted ADME and physicochem. properties. Taken together, compounds I and II could be selected for further modification and preclin. evaluation. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Quality Control of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate).
tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Quality Control of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics