Qian, Jianqiang published the artcileDesign and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy, Application of 2,3-Dimethoxybenzaldehyde, the main research area is benzylidenecyclohexenone preparation antitumor apoptosis autophagy thioredoxin reductase inhibitor; trimethoxybenzylidene dihydropyridinone preparation antitumor apoptosis autophagy thioredoxin reductase inhibitor; Antitumor activities; Benzylidenecyclohexenones; Piperlongumine; Reactive oxygen species (ROS); Thioredoxin reductase (TrxR).
Oxidative therapy, a strategy that specifically increases reactive oxygen species (ROS) levels in tumor cells by disrupting the redox homeostasis has gained increasing interest. The antitumor effects of the natural product piperlongumine (PL) appear to result from its ability to increase intracellular ROS levels via inhibition of antioxidative thioredoxin reductase (TrxR). Twenty-seven benzylidenecyclohexenone-based PL analogs (I [R = 3,4,5-trimethoxyphenyl, 1-acetyl-1H-indol-3-yl, 2H-1,3-benzodioxol-5-yl, etc.; R1 = H, I] and II [R2 = H, (benzyloxy)carbonyl, methanesulfonyl, phenylsulfonyl, p-toluenesulfonyl]) were designed, synthesized and evaluated for their pharmacol. properties. Most of the compounds exhibited potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. One of the most promising analogs I (R = 4-(trifluoromethoxy)phenyl; R1 = H (III)) showed 12-fold higher inhibitory activity against the thioredoxin reductase (TrxR) than PL and suppressed the expression of TrxR1 protein in breast cancer cells and inhibited TrxR enzymic activity. In addition, III increased ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. Compound III also triggered the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins. Finally, III displayed low acute toxicity and good inhibitory potency to tumors in mice. Overall, III is a promising anti-breast cancer candidate warranting further investigation.
European Journal of Medicinal Chemistry published new progress about Aldol condensation, stereoselective. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application of 2,3-Dimethoxybenzaldehyde.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem