Istituto di Cristallografia - CNR

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

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 17?-hydroxysteroid dehydrogenase type 1 (17?-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 17?-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 17?-HSD2 was investigated, revealing a rational approach for the design of selective inhibitors. 17?-HSD1 and 1 hold promise in fighting NSCLC.

ACS medicinal chemistry letters
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Emanuele M. Gargano, Abdelrahman Mohamed, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi, Hanna Drzewiecka, Pawe? P. Jagodzi?ski, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke, Orazio Nicolotti, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, and Martin Frotscher