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Updated: Feb 3, 2026

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In silico identification and in vitro validation of nogalamycin N-oxide (NSC116555) as a potent anticancer compound

Phongphat Obounchoey1, Lueacha Tabtimmai2, Praphasri Suphakun2

  • 1Interdisciplinary Program in Genetic Engineering, Graduate School, Kasetsart University, Chatuchak, Bangkok, Thailand.

Journal of Cellular Biochemistry
|October 17, 2018
PubMed

Insights

Researchers screened for new epidermal growth factor receptor (EGFR) inhibitors using computational methods. One compound, NSC116555, showed potent anti-cancer activity against lung cancer cells, inducing apoptosis.

Area of Science:

  • Oncology
  • Pharmacology
  • Computational Chemistry

Background:

  • Epidermal growth factor receptor (EGFR) overexpression is common in various cancers, particularly lung cancer.
  • Developing effective EGFR inhibitors is crucial for cancer therapy.

Purpose of the Study:

  • To virtually screen for novel human EGFR inhibitors.
  • To identify potent compounds with therapeutic potential against EGFR-driven cancers.

Main Methods:

  • Utilized the GOLD docking algorithm for virtual screening of the NCI database.
  • Tested 34 hit compounds for EGFR-tyrosine kinase (TK) inhibition.
  • Performed cell cytotoxicity assays on non-small-cell lung cancer (A549) cell line.

Main Results:

  • Identified two potent EGFR-TK inhibitors: NSC125910 (IC50 = 16.14 nM) and NSC116555 (IC50 = 37.71 nM).
  • NSC116555 exhibited significant cytotoxicity against A549 cells (IC50 = 0.19 µM), surpassing gefitinib's potency.
  • NSC116555 induced apoptosis in A549 cells in a dose-dependent manner.

Conclusions:

  • NSC116555 is a promising novel inhibitor of EGFR-TK with demonstrated cytotoxic and apoptosis-inducing effects against non-small-cell lung cancer.
  • This study highlights the potential of computational screening in discovering new anti-cancer drug candidates.
Keywords:
cancerdockingepidermal growth factor receptor-tyrosine kinasein silicoinhibitorsnogalamycin N-oxide

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