Design, synthesis and biological evaluation of hydrazone derivatives as anti-proliferative agents.

A series of triaryl-substituted hydrazones as structural acyclic prototypes were synthesized and screened for anti-proliferative activity against breast (Michigan cancer foundation-7 and MD Anderson metastatic breast-231) and uterine cancer (Ishikawa) cell lines. Two compounds were found to be the most active, 5e showed the maximum inhibition of both functional estrogen receptor containing Michigan cancer foundation-7 cells (IC: 7.8 µM) and Ishikawa cells (IC: 7.3 µM) whereas, compound 5i was selectively most active against ER-negative MD Anderson metastatic breast-231 cells (IC: 4.7 µM). The inhibitory effect of 5e in breast cancer and uterine cancer cells was due to ER antagonistic action, also supported by molecular docking studies. [ABSTRACT FROM AUTHOR]