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


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
09 Dec 2021
Historique:
received: 27 08 2021
accepted: 11 11 2021
entrez: 17 12 2021
pubmed: 18 12 2021
medline: 18 12 2021
Statut: epublish

Résumé

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

Identifiants

pubmed: 34917255
doi: 10.1021/acsmedchemlett.1c00462
pmc: PMC8667298
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1920-1924

Informations de copyright

© 2021 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare the following competing financial interest(s): A.S.A., C.J.v.K., S.M.-O., R.W.H., and M.F. are inventors of a US patent covering compounds 1-10 (US9884839(B2)).

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Auteurs

Emanuele M Gargano (EM)

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

Abdelrahman Mohamed (A)

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.
Pharmaceutical Organic Chemistry Department, Assiut University, Assiut 71526, Egypt.

Ahmed S Abdelsamie (AS)

Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Campus E81, D-66123 Saarbrücken, Germany.
Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, Cairo 12311, Egypt.

Giuseppe F Mangiatordi (GF)

Dipartimento di Farmacia Scienze del Farmaco, Università degli Studi di Bari, V. Orabona 4, I-70125 Bari, Italy.

Hanna Drzewiecka (H)

Department of Biochemistry and Molecular Biology, Poznan University of Medical Sciences, Świȩcickiego 6 Street, 60-781 Poznan, Poland.

Paweł P Jagodziński (PP)

Department of Biochemistry and Molecular Biology, Poznan University of Medical Sciences, Świȩcickiego 6 Street, 60-781 Poznan, Poland.

Arcangela Mazzini (A)

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

Chris J van Koppen (CJ)

ElexoPharm GmbH, Campus A12, D-66123 Saarbrücken, Germany.

Matthias W Laschke (MW)

Institute for Clinical and Experimental Surgery, Saarland University, D-66421, Homburg, Saar, Germany.

Orazio Nicolotti (O)

Dipartimento di Farmacia Scienze del Farmaco, Università degli Studi di Bari, V. Orabona 4, I-70125 Bari, Italy.

Angelo Carotti (A)

Dipartimento di Farmacia Scienze del Farmaco, Università degli Studi di Bari, V. Orabona 4, I-70125 Bari, Italy.

Sandrine Marchais-Oberwinkler (S)

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

Rolf W Hartmann (RW)

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.
Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Campus E81, D-66123 Saarbrücken, Germany.

Martin Frotscher (M)

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

Classifications MeSH