The synthesis of polysubstituted imidazopyridines and imidazopyrazines through the orthogonal union of Groebke-Blackburn and Ugi reactions is described . These motifs were produced efficiently in a tandem operation without intermediate isolation.  The synthesized scaffolds were biologically evaluated and found to posses potent anticancer and antibacterial activities. Importantly, some of these motifs (e.g. compound 5  ) were found to possess specific anti-breast cancer activity and others (e.g. compound 15  ) possess specific effects against melanoma cancer cell line (M8). Interestingly, the introduction of imidazobenzothiazole framework produced very potent anticancer compounds (e.g. compounds 29  and 33  ). These findings, however, form the foundation for further investigation in our continuing efforts to develop selective anticancer and antibacterial agents.

Tandem multicomponent reactions toward the design and synthesis of novel anticancer and antibacterial motifs

245th National Meeting (2013)

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