17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.
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AuthorsGargano, Emanuele M
Abdelsamie, Ahmed S
Mangiatordi, Giuseppe F
Jagodziński, Paweł P
van Koppen, Chris J
Laschke, Matthias W
Hartmann, Rolf W
MetadataShow full item record
AbstractIn the face of the clinical challenge posed by non-small cell lung cancer (NSCLC), the present need for new therapeutic approaches is genuine. Up to now, no proof existed that 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a viable target for treating this disease. Synthesis of a rationally designed library of 2,5-disubstituted furan derivatives followed by biological screening led to the discovery of 17β-HSD1 inhibitor 1, capable of fully inhibiting human NSCLC Calu-1 cell proliferation. Its pharmacological profile renders it eligible for further in vivo studies. The very high selectivity of 1 over 17β-HSD2 was investigated, revealing a rational approach for the design of selective inhibitors. 17β-HSD1 and 1 hold promise in fighting NSCLC.
CitationACS Med Chem Lett. 2021 Nov 18;12(12):1920-1924. doi: 10.1021/acsmedchemlett.1c00462.
AffiliationHIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany.
JournalACS medicinal chemistry letters
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