Synthesis and antimitotic activity of 2-phenyl-6-pyridinyl-2H-pyrazolo[4,3-c]pyridines

Abstract

An efficient synthetic route to 2-phenyl-6-pyridinyl-2H-pyrazolo[4,3-c]pyridines, alongside comprehensive structural elucidation and biological evaluation, is reported. Among the newly synthesized compounds, 7f, which contains 4-fluorophenyl and pyridin-2-yl substituents at the 2- and 6-positions, respectively, exhibited the strongest submicromolar cytotoxicity across various cancer cell lines. This compound compromised microtubule integrity, induced mitotic defects and aberrant cytokinesis, triggered endoreduplication, and ultimately resulted in cell death. Our findings highlight the potential of these pyrazolo[4,3-c]pyridine derivatives as antimitotic agents, providing a basis for further development of anticancer therapeutics.