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Medicinal Chemistry Research

, Volume 26, Issue 7, pp 1459–1468 | Cite as

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

  • Ravi Shankar
  • Ravindra K. Rawal
  • Uma S. Singh
  • Preeti Chaudhary
  • Rituraj Konwar
  • Kanchan Hajela
Original Research

Abstract

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.

Keywords

Hydrazones Estrogen receptor Antagonists Anti-proliferative Anti-cancer 

Notes

Acknowledgements

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.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

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Copyright information

© Springer Science+Business Media New York 2017

Authors and Affiliations

  • Ravi Shankar
    • 1
    • 2
  • Ravindra K. Rawal
    • 3
  • Uma S. Singh
    • 1
  • Preeti Chaudhary
    • 4
  • Rituraj Konwar
    • 4
  • Kanchan Hajela
    • 1
  1. 1.Medicinal & Process Chemistry Division,CSIR-Central Drug Research InstituteLucknowIndia
  2. 2.Medicinal Chemistry Division, CSIR-Indian Institute of Integrative MedicineJammuIndia
  3. 3.Department of Pharmaceutical ChemistryIndo-Soviet College of PharmacyMogaIndia
  4. 4.Endocrinology Division, CSIR-Central Drug Research InstituteLucknowIndia

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