Rh(III)-Catalyzed Redox-Neutral [4+2] Annulation for Direct Assembly of 3-Acyl Isoquinolin-1(2H)-ones as Potent Antitumor Agents.
Mengyao BianLei MaMin WuLiexin WuHui GaoWei YiChao ZhangZhi ZhouPublished in: ChemPlusChem (2019)
By virtue of an efficient rhodium(III)-catalyzed redox-neutral C-H activation/ring-opening of a strained ring/[4+2] annulation cascade of N-methoxybenzamides with propargyl cycloalkanols, diverse 3-acyl isoquinolin-1(2H)-ones were directly obtained in good yields and with excellent functional group compatibility. Additionally, their antitumor activities against various human cancer cells including HepG2, A549, MCF-7 and SH-SY5Y were evaluated and the action mechanism of the selected compound was also investigated in vitro. The results revealed that these products possessed a potent efficacy, by inhibiting proliferation and inducing apoptosis in a time-dependent and dose-dependent manner, suggesting that such compounds can serve as promising candidates for anti lung cancer drug discovery.
Keyphrases
- drug discovery
- room temperature
- signaling pathway
- endothelial cells
- fatty acid
- oxidative stress
- endoplasmic reticulum stress
- cell cycle arrest
- breast cancer cells
- induced pluripotent stem cells
- cell death
- single cell
- pluripotent stem cells
- electron transfer
- atomic force microscopy
- pi k akt
- cell proliferation
- ionic liquid