Li, Baicun published the artcileDiscovery of a Nur77-mediated cytoplasmic vacuolation and paraptosis inducer (4-PQBH) for the treatment of hepatocellular carcinoma, HPLC of Formula: 86-51-1, the main research area is quinoline amino benzoylhydrazide preparation diastereoselective cytoplasmic vacuolation paraptosis docking; 4-(Quinoline-4-amino) Benzoylhydrazide; Cytoplasmic vacuolation; Hepatocellular Carcinoma; Nur77; Paraptosis.
A series of 4-(quinoline-4-amino) benzoylhydrazide derivatives I (R = Ph, 3-bromo-4-methoxyphenyl, 3-bromothiophene-2-yl, 2-chloropyridin-3-yl, etc.) was synthesized and evaluated for their anti-HCC activity and binding affinity to Nur77 in vitro. Compound I (R = pyridin-4-yl) emerged as the best Nur77 binder (KD = 1.17μM) and has potentially selective cytotoxicity to HCC cells. Mechanistically, I (R = pyridin-4-yl) extensively induced caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy. Moreover, I (R = pyridin-4-yl) exhibited an effective xenograft tumor inhibition by modulating Nur77-dependent cytoplasmic vacuolation and paraptosis. This paper is the first to disclose that chemotherapeutic agents targeting Nur77-mediated cytoplasmic vacuolization and paraptosis may provide a promising strategy to combat HCC that frequently evade the apoptosis program.
Bioorganic Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, HPLC of Formula: 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem