Design, synthesis and biological evaluation of hydrazone derivatives as anti-proliferative agents
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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 (IC50: 7.8 µM) and Ishikawa cells (IC50: 7.3 µM) whereas, compound 5i was selectively most active against ER-negative MD Anderson metastatic breast-231 cells (IC50: 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.
KeywordsHydrazones Estrogen receptor Antagonists Anti-proliferative Anti-cancer
The authors, RS and USS are grateful to CSIR for Senior research fellowships and to the Ministry of Health & Family Welfare for financial assistance for the biological screening of compounds. All the authors are thankful to Sophisticated Analytical Instrument Facility for spectroscopic analyses of the pure compounds.
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Conflict of interest
The authors declare that they have no competing interests.
- Shankar R, Chakravarti B, Singh US, Ansari MI, Deshpande S, Dwivedi SKD, Bid HK, Konwar R, Kharkwal G, Chandra V, Dwivedi A, Hajela K (2009) Synthesis and biological evaluation of 3,4,6-triaryl-2-pyranones as a potential new class of anti-breast cancer agents. Bioorg Med Chem 17:3847–3856CrossRefPubMedGoogle Scholar