Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents

The preliminary results describe synthesis of a series of novel 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogs using hybrid approach employing copper(I)-catalyzed azide-alkyne cycloaddition and their evaluation as antiproliferative agents against four cancer cell lines by MTT assay. Among the synthesized compounds, 7g and 7h showed good activity against all the test cell lines. In particular, 7g (IC50 = 9.73 ± 4.09 µM) exhibited excellent activity against THP1 cancer cell line, and 7h (IC50 = 7.22 ± 0.32 µM) emerged as more active compound than the standard drug etoposide against HL60 cancer cell line.