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

Gurleen Kaur, Mohinder P. Mahajan, Manoj K. Pandey, Parvesh Singh, Srinivasa R. Ramisetti, Arun K. Sharma

Research output: Contribution to journalArticle

15 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)211-218
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume86
DOIs
StatePublished - Oct 30 2014

    Fingerprint

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this