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Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
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Small Molecular Leads Differentially Active Against HER2 Positive and Triple Negative Breast Cancer Cell Lines

Adnan Badran1, Atia-Tul-Wahab2, Sharmeen Fayyaz3

  • 1Faculty of Pharmacy and Medicinal Sciences, University of Petra, Amman 1194, Jordan.

Medicinal Chemistry (Shariqah (United Arab Emirates))
|November 7, 2018
PubMed
Abstract

Insights

Small molecules show promise for treating HER2-amplified and triple-negative breast cancers. Convallatoxin demonstrated potent activity against both cancer cell lines in vitro, highlighting potential therapeutic agents.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Breast cancer is the most common cancer in women globally, with distinct subtypes.
  • HER2 oncogene amplification drives aggressive growth and metastasis in certain breast cancers.
  • HER2 receptor protein on cell surfaces regulates cell growth.

Purpose of the Study:

  • To evaluate and compare the anti-breast cancer effects of commercially available compounds.
  • To assess compounds against HER2-overexpressing (BT-474) and triple-negative (MDA-MB-231) breast cancer cell lines.

Main Methods:

  • In vitro cell viability assays were performed.
  • Commercially available compounds were screened.
  • Activity was assessed against BT-474 and MDA-MB-231 breast cancer cell lines.

Main Results:

  • Six lead molecules with anti-breast cancer activity were identified.
  • Convallatoxin (4) exhibited potent activity (IC50: 0.63–0.69 µM) against both cell lines.
  • Phenol derivative (3) and Reserpine (5) selectively inhibited BT-474 and MDA-MB-231 cells, respectively.

Conclusions:

  • Small molecules demonstrate potential for treating HER2-amplified breast cancer.
  • Small molecules show potential for treating triple-negative breast cancer.
  • In vitro results highlight promising therapeutic agents for specific breast cancer subtypes.
Keywords:
Anti-cancerHuman Epidermal Growth Factor Receptor-2 (HER2)breast cancerconvallatoxinestrogen receptorsheterocyclic compounds.

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