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Updated: Feb 10, 2026

Imaging of Estrogen Receptor-α in Rat Pial Arterioles using a Digital Immunofluorescent Microscope
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A trisubstituted pyrazole derivative reduces DMBA-induced mammary tumor growth in rats by inhibiting estrogen

Hanumappa Ananda1, Kothanahally S Sharath Kumar2, Muddenahalli S Sudhanva1

  • 1Adichunchanagiri Institute for Molecular Medicine, Adichunchanagiri Institute of Medical Sciences, BG Nagara, Mandya, 571448, India.

Molecular and Cellular Biochemistry
|May 20, 2018
PubMed

Insights

A novel pyrazole derivative, compound 5d, effectively inhibits mammary carcinoma cell growth. This compound acts as an estrogen receptor alpha (ER-α) antagonist, reducing ER-α expression in tumor cells.

Area of Science:

  • Oncology
  • Endocrinology
  • Medicinal Chemistry

Background:

  • Aberrant estrogen receptor alpha (ER-α) expression is linked to breast cancer, endometrial cancer, and osteoporosis.
  • ER-α promotes breast cancer progression and resistance to chemotherapy and radiotherapy by increasing anti-apoptotic proteins.

Purpose of the Study:

  • To evaluate the anti-cancer potential of the synthetic pyrazole derivative, compound 5d.
  • To investigate the mechanism of action of compound 5d, specifically its interaction with ER-α.

Main Methods:

  • In vitro cytotoxicity assays against mammary carcinoma cells.
  • Molecular docking studies to predict binding of compound 5d to the ER-α ligand binding domain.
  • In vivo studies using immunohistochemistry and quantitative RT-PCR to assess ER-α expression in tumor cells after treatment.

Main Results:

  • Compound 5d demonstrated significant cytotoxicity against mammary carcinoma cells.
  • Molecular docking indicated that compound 5d binds to the ligand binding domain of ER-α.
  • In vivo studies confirmed a reduction in ER-α expression in tumor cells treated with compound 5d, suggesting an antagonistic effect.

Conclusions:

  • Compound 5d is a potent inhibitor of mammary carcinoma cells.
  • The study identifies compound 5d as a potential ER-α antagonist with therapeutic implications for ER-α-driven cancers.
Keywords:
DMBA (7,12-Dimethylbenzanthracene)ER-αPyrazoleSERM’sSprague–Dawley

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