Design, synthesis and biological evaluation of 3-arylisoquinoline derivatives as topoisomerase I and II dual inhibitors for the therapy of liver cancer was written by Deng, Xuemei;Luo, Tian;Zhang, Xi;Li, Yuehua;Xie, Liming;Jiang, Weifan;Liu, Linyi;Wang, Zhen. And the article was included in European Journal of Medicinal Chemistry in 2022.COA of Formula: C7H16N2 This article mentions the following:
To explore novel topoisomerase inhibitors with high activity and druggability, 3-aryl isoquinoline alkaloids based on the corydamine modification and preliminary SARs of isoquinoline alkaloids in our previous works were re-designed. Currently, the design strategy is mainly revolved around the rigidity and flexibility of the mol. side chain and the mol. size. Consequently, not only the activity and druggability of the compound could be further improved, also the mechanism behind could been discovered. In vitro pharmacol. studies, the outstanding nature with the excellent activity and the researchable depth of azepane-substituted compound has been found through the vitro cytotoxicity test (IC50 = 1.93μM in HuH7 cells and 2.10μM in LM9 cells) and topoisomerase test. It was found that azepane-substituted compound had dual inhibitory effects on topoisomerase I and II, and its inhibitory activity on topoisomerase II is stronger than the pos. drug etoposide. From the perspective of mol. docking, it had been verified that azepane-substituted compound could insert between DNA base pairs, which was consistent with the results of the DNA unwinding experiment Meanwhile, azepane-substituted isoquinoline could inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Therefore, this study may lay a foundation for the discovery of 3-arylisoquinoline compounds with anti-liver cancer potential. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1COA of Formula: C7H16N2).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.COA of Formula: C7H16N2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics