Yanwen Lv

Synthesis, molecular docking and biological evaluation of quinolone derivatives as novel anticancer agents

A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines, human lung carcinoma cell (A549), human promyelocytic leukemia cell (HL-60), and human cervical cancer cell (Hela). Compound 8i was found to be 5-times more potent in cell-killing activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 µM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-topoisomerase I.

A continuous-flow fischer indole synthesis of 3-methylindole in an ionic liquid

A continuous-flow reactor (Corning G1 reactor) was hereby introduced for Fischer indole synthesis of 3-methylindole by reaction of phenyl hydrazines and propylaldehyde. Stoichiometric Lewis acid, ZnCl2, was supplied as catalyst as well as remover of NH3 which generated during the indole ring formation. Ionic liquid ([EMIM][BF4]) was employed as solvent according to its high-temperature tolerance and good product distribution. After a straightforward extraction process, 3-methylindole could be obtained in a 95.3% yield (96.0% purity) under optimized conditions. Ionic liquid (IL) was then recovered by another extraction process, and the recovered IL acted nearly as efficiently as new IL for this Fischer indole reaction.