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 published an article on February 5 ,2022. The article was titled 《Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer》, and you may find the article in European Journal of Medicinal Chemistry.Related Products of 39546-32-2 The information in the text is summarized as follows:
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. The experimental process involved the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Related Products of 39546-32-2)
Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Related Products of 39546-32-2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem