Novel orthodiphenyl five-member N-heteroaromatic compounds as potent anticancer cell agents

A series of diphenyl-N-heteroaromatic compounds were designed, synthesized, and evaluated for anticancer efficacies (antimigration and antiproliferation) against human cancer cell lines. The favorable 2H-1,2,3-triazole compound 4a was optimized, leading to the discovery of compounds 4b and 4c with more potent antimigratory and antiproliferative activities. The transwell assay showed that compounds 4b and 4c dose-independently inhibited the migration of the two cancer cell lines (human breast cancer cell line MDA-MB-231 and pancreatic cancer cell line PANC1) with the low IC₅₀ values of 0.24 and 0.47 µM, respectively. The sulforhodamine-B (SRB) assay showed that compounds 4b and 4c inhibited the proliferation of PANC1 cells with the IC₅₀ values 0.86 µM and 1.41 µM, respectively. These results indicate that compounds 4b and 4c with 1,2,3-triazole scaffold may be further developed as potent anticancer agents in the future. [Figure not available: see fulltext.]