80221-41-6Relevant academic research and scientific papers
Ethyl lactate-involved three-component dehydrogenative reactions: Biomass feedstock in diversity-oriented quinoline synthesis
Wan, Jie-Ping,Yang, Lu
supporting information, p. 3074 - 3078 (2020/06/25)
Three-component reactions of ethyl/methyl lactate, anilines and aldehydes providing quinolines have been developed via simple iron(iii) chloride catalysis without using an additional organic medium or external oxidant. This three-component protocol shows
New quinoline/chalcone hybrids as anti-cancer agents: Design, synthesis, and evaluations of cytotoxicity and PI3K inhibitory activity
Abbas, Samar H.,Abd El-Hafeez, Amer Ali,Shoman, Mai E.,Montano, Monica M.,Hassan, Heba A.
, p. 360 - 377 (2018/11/23)
A series of quinoline-chalcone hybrids was designed as potential anti-cancer agents, synthesized and evaluated. Different cytotoxic assays revealed that compounds experienced promising activity. Compounds 9i and 9j were the most potent against all the cell lines tested with IC50 = 1.91–5.29 μM against A549 and K-562 cells. Mechanistically, 9i and 9j induced G2/M cell cycle arrest and apoptosis in both A549 and K562 cells. Moreover, all PI3K isoforms were inhibited non selectively with IC50s of 52–473 nM when tested against the two mentioned compounds with 9i being most potent against PI3K-γ (IC50 = 52 nM). Docking of 9i and 9j showed a possible formation of H-bonding with essential valine residues in the active site of PI3K-γ isoform. Meanwhile, Western blotting analysis revealed that 9i and 9j inhibited the phosphorylation of PI3K, Akt, mTOR, as well as GSK-3β in both A549 and K562 cells, suggesting the correlation of blocking PI3K/Akt/mTOR pathway with the above antitumor activities. Together, our findings support the antitumor potential of quinoline-chalcone derivatives for NSCLC and CML by inhibiting the PI3K/Akt/mTOR pathway.
