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Topoisomerases I and II are nuclear enzymes that play crucial roles in DNA metabolism such as replication, transcription, recombination, repair, chromatin assembly, and chromosome segregation. Due to the crucial role of topoisomerases in the maintenance and replication of DNA during proliferation, cells become highly vulnerable when these functions are lost. Consequently, topo I and II have been attractive targets for design of antitumor agents. It has been reported in our research group α-terpyridine derivatives showed strong cytotoxicities against several human cancer cell lines and considerable topo I and II inhibitory activities. We also studied for topo I and II inhibitory activities of 2,6-dithienyl-4-furylpyridines. From the previous structure-activity relationship studies, we found 2,6-dithienyl-4-furylpyridines exhibited strong topo I and II inhibitory activities as well as strong cytotoxicity against several human cancer cell lines. It would be very interesting to prepare 2,6-dithienyl-4-arylpyridines and evaluate topo I and II inhibitory activities of the prepared compounds. In addition, the comparison of activities between two moieties may provide valuable information for the development of novel antitumor agents. In connection with previous studies, 2,6-dithienyl-4-arylpyridines were prepared and evaluated for their topo I and II inhibitory effects (Figure 1). Experimental Section

2,6-Dithienyl-4-arylpyridines: Synthesis, Topoisomerase I and II Inhibition and Structure-activity Relationship