Song, Jing-Ru; Li, Na; Li, Dian-Peng published the artcile< Synthesis and anti-proliferation activity of Mogrol derivatives bearing quinoline and triazole moieties>, Name: 3-Aminoisonicotinaldehyde, the main research area is Mogrol quinolinyl triazolyl synthesis antitumor agent; Lung cancer; Mogrol; Quinoline; Structural modification; Triazole.
A series of novel derivatives based on Mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47μM against A549 cell, and could induce the cell apoptosis in a dose-dependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with Mogrol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13μM. The research stimulated the development of potential therapeutic agent for lung cancer from the natural Mogrol.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 55279-29-3 belongs to class pyridine-derivatives, and the molecular formula is C6H6N2O, Name: 3-Aminoisonicotinaldehyde.