In 2019,European Journal of Medicinal Chemistry included an article by Yao, Bin-Rong; Sun, Yue; Chen, Shuang-Long; Suo, Hao-Dong; Zhang, Yu-Long; Wei, Hao; Wang, Chun-Hua; Zhao, Feng; Cong, Wei; Xin, Wen-Yu; Hou, Gui-Ge. Related Products of 1445-73-4. The article was titled 《Dissymmetric pyridyl-substituted 3,5-bis(arylidene)-4-piperidones as anti-hepatoma agents by inhibiting NF-κB pathway activation》. The information in the text is summarized as follows:
A series of dissym. pyridyl-substituted 3,5-bis(arylidene)-4-piperidones (BAPs, I [R1 = 3-pyridinyl, 4-pyridinyl; R2 = 2-F, 4-cyano, 3,4,5-OMe, etc.] II[R3 = 3-pyridinyl, 4-pyridinyl; R4 = F, CF3; R5 = H, Cl, CF3, etc]) were designed and synthesized to get new anti-hepatoma agents with anti-inflammatory activity and hypotoxicity. Many of them exhibited potential anti-hepatoma properties against human hepatocellular carcinoma cell lines (HepG2, QGY-7703, SMMC-7721) and hypotoxicity for human normal heptical cell line (HHL-5, LO2) and prominently inhibited lipopolysaccharides (LPS) induced IL-6, TNF-α secretion to exert its anti-inflammatory effect. Combining the data of cytotoxicity, cytocompatibility and anti-inflammatory activity, II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be the potential anti-hepatoma agent. II [R3 = 3-pyridinyl; R4 = R5 = CF3] effectively promoted cell apoptosis through up-regulating cleaved caspase-3 and Bax expression and down-regulating Bcl-2 expression. Furthermore, II [R3 = 3-pyridinyl; R4 = R5 = CF3]prominently inhibited NF-κB pathway activation by blocking the phosphorylation of IκBα, p65 and the nuclear translocation of NF-κB induced by TNF-α and LPS. In addition, II [R3 = 3-pyridinyl; R4 = R5 = CF3] could reasonably bind to the active site of Bcl-2 and NF-κB/p65 protein proved by Mol. docking analyses. Moreover, II [R3 = 3-pyridinyl; R4 = R5 = CF3] significantly suppressed the growth and inflammatory response of HepG2 xenografts in nude mice and was relatively nontoxic to mice. These results suggested that II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be effective and hypotoxicity anti-hepatoma agent for the clin. treatment of liver cancers. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Related Products of 1445-73-4)
1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 1445-73-4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem