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

► Synthesized and characterized the novel derivatives of (R/S)-2-[2-hydroxy-3-(4-phenylpiperazin-1-yl) propyl]-1H-pyrrolo [3,4-b] quinolin-3(2H)-one in good to excellent yields. ► Synthesized racemic derivatives were resolved by using Candida antarctica B (CAL-B) and Candida rugosa (CRL) Lipases. ► All newly synthesized and resolved isomers were evaluated for their antitumor activity against cancer cells such as human neuroblastoma SK-N-SH and human lung carcinoma A549 cell lines. ► The results have shown that the compound 1 S-(−) alcohol was more effective in inhibiting the tumor cell growth.