2. Academic Validation
  3. Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents

Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents

  • Eur J Med Chem. 2014 Oct 30:86:211-8. doi: 10.1016/j.ejmech.2014.08.050.
Gurleen Kaur 1,  Mohinder P Mahajan 2,  Manoj K Pandey 3,  Parvesh Singh 4,  Srinivasa R Ramisetti 3,  Arun K Sharma 3
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, Apeejay Stya University, Plot No. 23, Institutional Area, Sector-32, Gurgaon 122001, India.
  • 2 School of Pharmaceutical Sciences, Apeejay Stya University, Plot No. 23, Institutional Area, Sector-32, Gurgaon 122001, India; Apeejay Stya Research Foundation, Plot No. 23, Institutional Area, Sector-32, Gurgaon 122001, India. Electronic address: mpmahajan@apeejay.com.
  • 3 Department of Pharmacology, Penn State Hershey Cancer Institute, CH72 Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
  • 4 School of Chemistry and Physics, University of Kwa-Zulu Natal (UKZN), Westville Campus, Durban 4000, South Africa.
PMID: 25164760 DOI: 10.1016/j.ejmech.2014.08.050
Abstract

The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast Cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast Cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Estrogen Receptor Modulators (SERMs) i.e. Ospemifene and Tamoxifen, against these cell lines. Compound 8 was relatively more cytotoxic to MCF-7 cells similar to Ospemifene and Tamoxifen, while most potent compounds 6 and 7 were equally effective in inhibiting growth of both ER-positive and ER-negative cell lines. The observed activity profiles were further supported by the docking studies performed against estrogen receptors (ERα and ERβ). Compounds 6, 7 and 8 exhibited stronger binding affinities with both ERα and ERβ compared to Ospemifene and Tamoxifen.

Keywords

Anti-breast cancer agents; Docking studies; Ospemifene; SERMs; Tamoxifen.

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