Abstract

The intramolecular regioselective aerobic oxidative cyclization via two types of discrete C–H activation in 7-chloroquinoline analogues is described. All the synthesized compounds are screened against three human cancer cell lines (CCRF-CEM, HT29, and MCF7) for their anticancer activities. Among them, chloroquine analogues with naphthalene ring either substituted/fused form enhance remarkable cytotoxic activity against human breast adenocarcinoma cancer cell line (MCF-7) which outranged positive control doxorubicin. Similarly, 3-chloro-7H,12H-pyrazolo[5,4-b]quinolino[3,2-c]indole has possessed significant activity against all the tested cell lines and outranged activity against CCRF-CEM cell line.

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