Guangzhou Municipal and Guangdong Provincial Key Laboratory of Protein Modification and Degradation & Molecular Target and Clinical Pharmacology State Key Laboratory of Respiratory Disease School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University Guangzhou, Guangdong, 511436, P. R. China.
Chempluschem. 2020 Mar;85(3):405-410. doi: 10.1002/cplu.201900616. Epub 2019 Dec 11.
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.
通过高效的铑(III)催化的氧化还原中性 C-H 活化/张力环开环/[4+2]环加成级联反应，N-甲氧基苯甲酰胺与丙炔环烷醇直接得到多种 3-酰基异喹啉-1(2H)-酮，产率高，官能团兼容性好。此外，还评价了它们对包括 HepG2、A549、MCF-7 和 SH-SY5Y 在内的多种人癌细胞的抗肿瘤活性，并在体外研究了选定化合物的作用机制。结果表明，这些产物具有很强的功效，能够通过时间和剂量依赖性抑制增殖并诱导细胞凋亡，这表明此类化合物可以作为有前途的候选物用于发现抗肺癌药物。
