Chemoenzymatic synthesis with lipase catalyzed resolution and evaluation of antitumor activity of (R/S)-2-(2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl)-1H-pyrrolo(3,4-b)quinolin-3( 2H)-one.

摘要

Synthesis, characterization, resolution and evaluation of novel (R/S)-2-2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl-1H-pyrrolo3,4-bquinolin-3( 2H)-one derivatives are described. Enantiomerically pure compounds were isolated in good to excellent yield with high enantiomeric excess under mild reaction conditions by using Candida antarctica B (CAL-B) and Candida rugosa (CRL) Lipases. Newly synthesized and resolved compounds were screened for their antitumor activity against cancer cells such as human neuroblastoma SK-N-SH and human lung carcinoma A549 cell line in vitro. The results have shown that the compound 1 S-(-) alcohol was more effective in inhibiting the tumor cell growth.