Synthesis and biological evaluation of novel benzo[a]pyridazino[3,4-c] phenazine derivatives

A convenient microwave-assisted one-pot four-component synthetic approach was developed en route to novel functionalized benzo[a]pyridazino[3,4-c]phenazine derivatives starting from 2-hydroxy-1,4-naphthoquinone, aromatic aldehydes, methyl hydrazine and o-phenylenediamine. Nine new derivatives were successfully synthesized and subsequently evaluated in terms of their biological profiles. The results revealed good cytotoxic activities of compounds 6a, 6h against KB, HepG2, Lu1 and MCF7 human cancer cell lines. Besides that, compound 6d exhibited promising antimicrobial activities toward Staphylococcuc aureus and Bacillus subtilis bacterial strains with IC50 < 6 mu M.

Automated summary

A convenient microwave-assisted one-pot four-component synthetic approach was developed to synthesize novel functionalized benzo[a]pyridazino[3,4-c]phenazine derivatives. Some of the synthesized compounds showed good cytotoxic activities against human cancer cell lines and promising antimicrobial activities against bacterial strains.