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Medicinal Chemistry Research

, Volume 24, Issue 5, pp 1842–1856 | Cite as

Synthesis, in-vitro screening, and docking analysis of novel pyrrolidine and piperidine-substituted ethoxy chalcone as anticancer agents

  • Santosh N. MokaleEmail author
  • Pritam N. Dube
  • Swati A. Bhavale
  • Ibrahim Sayed
  • Afreen Begum
  • Manjusha C. Nevase
  • Vishakha R. Shelke
  • Abdul Mujaheed
Original Research

Abstract

A series of novel-substituted chalcone analogs were synthesized and evaluated for antiproliferative activity against estrogen receptor-positive MCF-7 breast cancer cell lines. Among the synthesized derivatives 4a, 5a, 5b, 5c, 5e, 5′a, and 5′d show good antiproliferative activity as compared to standard tamoxifen. The study highlighted the advantage of introducing the amine side chain pharmacophore in substituted chalcone enhances the anticancer potential. The study also suggests that these analogs can serve as better therapeutic agents against breast cancer and can provide starting point for building more potent analogs in future. The binding mechanism and ADME properties of target compounds were analysed using Schrödinger software.

Keywords

Chalcone Breast cancer Molecular docking ADME 

Notes

Acknowledgments

The authors are thankful to Tata Memorial Centre-Advanced Centre for Treatment, Research and Education in Cancer (ACTREC) Kharghar, Navi Mumbai for in-vitro assay against breast cancer activity. This work was supported by the Department of Science and Technology (DST), New Delhi, India (Project File No. SR/FT/LS-132/2012 & Sanction Diary No. SERB/F/4302/2012-13).

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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  • Santosh N. Mokale
    • 1
    Email author
  • Pritam N. Dube
    • 1
  • Swati A. Bhavale
    • 1
  • Ibrahim Sayed
    • 1
  • Afreen Begum
    • 1
  • Manjusha C. Nevase
    • 1
  • Vishakha R. Shelke
    • 1
  • Abdul Mujaheed
    • 1
  1. 1.Department of Pharmaceutical ChemistryY.B. Chavan College of PharmacyAurangabadIndia

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