Qian, Yuqing published the artcileDesign and synthesis of N-(1-(6-(substituted phenyl)-pyridazin-3-yl)-piperidine-3-yl)-amide derivatives as JMJD6 inhibitors, Quality Control of 73874-95-0, the main research area is pyridazinyl piperidinyl amide preparation antitumor inhibitor docking; Breast cancer, antitumor agent; JMJD6 inhibitor.
JMJD6 is a member of the JmjC domain-containing family and has been identified as a promising therapeutic target for treating estrogen-induced and triple-neg. breast cancer. To develop novel anti-breast cancer agents, a class of N-(1-(6-(substituted phenyl)-pyridazine-3-yl)-piperidine-3-yl)-amide derivatives I [R = 3-(pyridin-3-ylcarbonylamino), 4-(4-methoxyphenylcarbonylamino), 3-(4-methoxyphenylcarbonylamino), etc.; R1 = MeO, Cl, Et, NH2, NHBoc, NHMe] as potential JMJD6 inhibitors was synthesized. Among them, the anti-cancer compound I [R = 3-((4-methoxyphenyl)amidyl), etc.; R1 = NHMe] was an excellent JMJD6 binder (KD = 0.75 ± 0.08μM). It could upregulate the mRNA and protein levels of p53 and its downstream effectors p21 and PUMA by inhibiting JMJD6. Besides, compound I [R = 3-(4-methoxyphenylcarbonylamino); R1 = NHMe] displayed potent anti-proliferative activities against tested breast cancer cells by the induction of cell apoptosis and cell cycle arrest. Significantly, compound I [R = 3-(4-methoxyphenylcarbonylamino); R1 = NHMe] also promoted a remarkable reduction in tumor growth, with a TGI value of 66.6% (50 mg/kg, i.p.). Taken together, this findings suggest that compound I [R = 3-(4-methoxyphenylcarbonylamino); R1 = NHMe] is a potent JMJD6 inhibitor bearing a new scaffold acting as a promising drug candidate for the treatment of breast cancer.
Bioorganic Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Quality Control of 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem