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17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer

Emanuele M Gargano1, Abdelrahman Mohamed1,2, Ahmed S Abdelsamie3,4

  • 1Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.

ACS Medicinal Chemistry Letters
|December 17, 2021
PubMed

Insights

Researchers discovered a novel 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitor, compound 1, which effectively halts non-small cell lung cancer (NSCLC) cell growth. This finding offers a promising new therapeutic strategy for NSCLC treatment.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Biochemistry

Background:

  • Non-small cell lung cancer (NSCLC) presents a significant clinical challenge requiring novel therapeutic strategies.
  • The role of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) as a therapeutic target in NSCLC was previously unestablished.

Purpose of the Study:

  • To identify and characterize novel inhibitors of 17β-HSD1 for potential NSCLC treatment.
  • To explore the potential of 17β-HSD1 as a viable drug target in NSCLC therapy.

Main Methods:

  • Rational design and synthesis of a library of 2,5-disubstituted furan derivatives.
  • Biological screening of synthesized compounds to identify 17β-HSD1 inhibitors.
  • Evaluation of cell proliferation inhibition in human NSCLC Calu-1 cells.

Main Results:

  • Discovery of compound 1, a potent 17β-HSD1 inhibitor.
  • Compound 1 demonstrated complete inhibition of human NSCLC Calu-1 cell proliferation.
  • Compound 1 exhibited high selectivity over the 17β-HSD2 enzyme, providing a basis for selective inhibitor design.

Conclusions:

  • 17β-HSD1 is a promising therapeutic target for non-small cell lung cancer.
  • Compound 1 is a potent and selective 17β-HSD1 inhibitor with potential for further in vivo investigation and development for NSCLC treatment.

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