Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer was written by Wu, Chun-Feng;Wang, Qing-Chen;Chen, Rui;Zhou, Hai-Ling;Wu, Ting-Ting;Du, Yao;Zhang, Na-Na;Zhang, Hui-Min;Fan, Zu-Yan;Wang, Li-Li;Hu, Chu-Jiao;Sang, Zhi-Pei;Li, Hong-Liang;Wang, Ling;Tang, Lei;Zhang, Ji-Quan. And the article was included in European Journal of Medicinal Chemistry in 2022.Quality Control of N,N-Dimethylpiperidin-4-amine This article mentions the following:
The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this study, a series of diaryl urea derivatives has been designed and synthesized based on clin. candidate gedatolisib, and most of the newly synthesized derivatives showed kinase inhibitory and antiproliferative activities within nanomolar and submicromolar level, resp. The terminal L-proline amide substituted derivative I showed 8.6-fold more potent PI3Kα inhibitory activity (0.7 nM) and 4.6-fold more potent antiproliferative effect against HCT116 cell lines (0.11μM) compared with control gedatolisib. The potential antitumor mechanism and efficacy of I in HCT116 xenograft models have also been evaluated, and found I showed comparable in vivo antitumor activity with gedatolisib. The safety investigations revealed that compound I exhibited more safer profiles in the selectivity of liver cells (selectivity index: >6.6 vs 1.85) and blood glucose regulation than gedatolisib. In addition, the in vitro stability assays also indicated that developed compound I possessed good metabolic stabilities. In the experiment, the researchers used many compounds, for example, N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6Quality Control of N,N-Dimethylpiperidin-4-amine).
N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Quality Control of N,N-Dimethylpiperidin-4-amine
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem