Zhang, Xiangyu; Huang, Hailan; Zhang, Ziheng; Yan, Jiangkun; Wu, Tianxiao; Yin, Wenbo; Sun, Yixiang; Wang, Xinran; Gu, Yanting; Zhao, Dongmei; Cheng, Maosheng published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors》.HPLC of Formula: 109-01-3 The article contains the following contents:
A series of benzofurans I [R = 3-aminopropylamino, pyrrolidin-3-ylamino, piperazin-1-yl, etc.; Ar = pyrimidin-5-yl, p-tolyl, 1-methylindazol-5-yl, etc.] were designed, synthesized and biochem. evaluated as LSD1 inhibitors based on scaffold hopping and conformational restriction strategy. Most of the compounds I potently suppressed the enzymic activities of LSD1 and potently inhibited tumor cells proliferation. In particular, the representative compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] exhibited excellent LSD1 inhibition at the mol. levels with IC50 = 0.065μM, as well as anti-proliferation against MCF-7, MGC-803, H460, A549 and THP-1 tumor cells with IC50 values of 2.90 ± 0.32, 5.85 ± 0.35, 2.06 ± 0.27, 5.74 ± 1.03 and 6.15 ± 0.49μM, resp. The binding modes of these compounds I were rationalized by mol. docking. Meanwhile, a preliminary druggability evaluation showed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] displayed favorable liver microsomal stability and weak inhibitory activity against CYPs at 10μM. Remarkably, H460 xenograft tumors studies revealed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] demonstrated robust in-vivo antitumor efficacy without significant side effects. All the results demonstrated that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] could represent a promising lead for further development. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..HPLC of Formula: 109-01-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics