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dc.contributor.authorGargano, Emanuele M
dc.contributor.authorMohamed, Abdelrahman
dc.contributor.authorAbdelsamie, Ahmed S
dc.contributor.authorMangiatordi, Giuseppe F
dc.contributor.authorDrzewiecka, Hanna
dc.contributor.authorJagodziński, Paweł P
dc.contributor.authorMazzini, Arcangela
dc.contributor.authorvan Koppen, Chris J
dc.contributor.authorLaschke, Matthias W
dc.contributor.authorNicolotti, Orazio
dc.contributor.authorCarotti, Angelo
dc.contributor.authorMarchais-Oberwinkler, Sandrine
dc.contributor.authorHartmann, Rolf W
dc.contributor.authorFrotscher, Martin
dc.date.accessioned2022-01-21T10:30:22Z
dc.date.available2022-01-21T10:30:22Z
dc.date.issued2021-11-18
dc.identifier.citationACS Med Chem Lett. 2021 Nov 18;12(12):1920-1924. doi: 10.1021/acsmedchemlett.1c00462.en_US
dc.identifier.issn1948-5875
dc.identifier.pmid34917255
dc.identifier.doi10.1021/acsmedchemlett.1c00462
dc.identifier.urihttp://hdl.handle.net/10033/623149
dc.description.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.en_US
dc.language.isoenen_US
dc.publisherACSen_US
dc.rightsAttribution 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/*
dc.title17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.en_US
dc.typeArticleen_US
dc.contributor.departmentHIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany.en_US
dc.identifier.journalACS medicinal chemistry lettersen_US
dc.source.volume12
dc.source.issue12
dc.source.beginpage1920
dc.source.endpage1924
dc.source.journaltitleACS medicinal chemistry letters
dc.source.countryUnited States


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Attribution 4.0 International
Except where otherwise noted, this item's license is described as Attribution 4.0 International