Yu, Jianjun; Xu, Lei; Hong, Duidui; Zhang, Xiaotuan; Liu, Jieyu; Li, Daqiang; Li, Jia; Zhou, Yubo; Liu, Tao published the artcile< Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors>, Related Products of 20744-39-2, the main research area is phenol ether preparation proteasome inhibitor antitumor SAR mol docking; Non-covalent; Non-peptide; Phenol ether; Proteasome inhibitor; Solid cancers.
A series of novel phenol ether derivatives I (n = 1, 2; R1 = Me, methoxy, n-Pr, etc.; R2 = 4-FC6H4, 2-naphthyl, 3-pyridinyl, etc.) were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound I (n = 1; R1 = n-Bu; R2 = pyridazine-4-yl) proved to be the most potent compound (chymotrypsin-like: IC50 = 49 nM), exhibiting a 2-fold higher potency compared to the reported PI-1840. Besides, compound I (n = 1; R1 = n-Bu; R2 = pyridazine-4-yl) exhibited excellent metabolic stability and selective anti-proliferative activity against solid cancer cell lines including HepG2 and HGC27, providing incentive for the further development as a potential anticancer agent against solid cancers.
European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Related Products of 20744-39-2.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem