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As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. The inhibitory activity of compounds 10-18 was determined against three cancer cell lines using the MTT colorimetric assay. The screening revealed that derivatives 16b and 17b exhibited significant cytotoxic activity against the gastric cancer cell line but was not active against a normal cell line, in contrast to doxorubicin, a standard chemotherapeutic drug in clinical use. Interestingly, no hemolytical activity was observed when the toxicity of 16b and 17b was tested against blood cells. The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells. [ABSTRACT FROM AUTHOR]

Herein, we report a direct diazenylation of active methylene compounds that is environmentally friendly, cost-effective, and scalable, utilizing a heterogeneous TiO 2 catalyst that is both accessible and recyclable. The scope of this transformation shows excellent compatibility with both electron-rich and electron-poor diazonium salts, yielding the desired products in very good yields at room temperature.