One-pot multicomponent synthesis of indole incorporated thiazolylcoumarins and their antibacterial, anticancer and DNA cleavage studies

Abstract A series of indole incorporated thiazolylcoumarins ( 7a – q ) have been synthesized and evaluated for their antibacterial, anticancer and DNA cleavage studies. Analysis of antibacterial studies indicated that all the synthesized compounds possess promising activity towards the screened bacterial strains. In vitro anticancerous action was studied for compound 7a (NSC: 768621/1) against the full panel of 60 human tumor cell lines. The five dose level activity results revealed that, the compound 7a was active against all the cell lines among them it has shown potent activity against Leukemia: CCRF-CEM (GI 50 : 0.33 μM), Non-Small Cell Lung Cancer: NCI-H522 (GI 50 : 1.03 μM), Colon Cancer: HCT-116 (GI 50 : 1.60 μM), CNS Cancer: SF-539 (GI 50 : 1.58 μM), Melanoma MALME-3M (GI 50 : 1.59 μM), Ovarian Cancer: OVCAR-3 (GI 50 : 1.16 μM), Renal Cancer: UO-31 (GI 50 : 0.76 μM), Prostate Cancer: PC-3 (GI 50 : 0.82 μM) and Breast Cancer: BT-549 (GI 50 : 1.13 μM). DNA cleavage studies revealed that even at 50 μg/mL concentration complete DNA digestion was observed for all the compounds, except for compound ( 7o ) where partial DNA digestion was observed even at 100 μg/mL.