Yang, Renjing published the artcileSynthesis and Anti-Hepatoma Activities of U12 Derivatives Arresting G0/G1 Phase and Inducing Apoptosis by PI3K/AKT/mTOR Pathway, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Pharmaceuticals (2022), 15(1), 107, database is CAplus and MEDLINE.
In this study, the structural modification and optimization of U12 were further investigated and twelve U12 derivatives I [R = aminocyclopropyl, piperazin-1-yl, 4-methylanilino, etc.], II were synthesized by substitution, esterification and amidation reactions. The evaluation of the cytotoxicity of synthetic derivatives against hepatoma cell lines (HepG2) indicated that II, I [R = 4-benzylpiperazin-1-yl, [4-[(E)-cinnamyl]piperazin-1-yl], piperazin-1-yl, aziridin-1-yl, 4-hydroxyanilino] showed more effective cytotoxic effects on the growth of HepG2 cells than U12, and the preliminary structure-activity relationship was discussed. Among them, compound I [R = 4-benzylpiperazin-1-yl] exhibited the most potent anti-hepatocellular carcinoma activity. Mechanism studies indicated that compound I [R = (4-benzylpiperazin-1-yl)] inhibited HepG2 cell proliferation by arresting the G0/G1 phase, and suppressed the activation of the PI3K/AKT/mTOR pathway. Further studies showed that compound I [R = 4-benzylpiperazin-1-yl] induced HepG2 cells apoptosis through activating the caspase signaling pathway. Furthermore, compound I [R = (4-benzylpiperazin-1-yl)] evidently inhibited the growth of HepG2-derived tumor xenografts in vivo without observable adverse effects. Thus, compound I [R = 4-benzylpiperazin-1-yl] might be considered as a promising candidate for the treatment of hepatocellular carcinoma.
Pharmaceuticals published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C4H11NO, Recommanded Product: (E)-1-Cinnamylpiperazine.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics