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17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.
Gargano, Emanuele M Mohamed, Abdelrahman Abdelsamie, Ahmed S Mangiatordi, Giuseppe F Drzewiecka, Hanna Jagodziński, Paweł P Mazzini, Arcangela van Koppen, Chris J Laschke, Matthias W Nicolotti, Orazio
Gargano, Emanuele M
Mohamed, Abdelrahman
Abdelsamie, Ahmed S
Mangiatordi, Giuseppe F
Drzewiecka, Hanna
Jagodziński, Paweł P
Mazzini, Arcangela
van Koppen, Chris J
Laschke, Matthias W
Nicolotti, Orazio
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2021-11-18
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Abstract
In 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.
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ACS Med Chem Lett. 2021 Nov 18;12(12):1920-1924. doi: 10.1021/acsmedchemlett.1c00462.
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en
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1948-5875
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Attribution 4.0 International