Issue 21, 2017

Structure-based optimisation of non-steroidal cytochrome P450 17A1 inhibitors

Abstract

Five new non-steroidal inhibitors for cytochrome P450 17A1 (CYP17A1) were identified by structure-based optimisation from a recently identified selective CYP17A1 inhibitor. The compounds are nanomolar inhibitors of steroidogenesis measured in recombinant CYP17A1 and in H295R cells.

Graphical abstract: Structure-based optimisation of non-steroidal cytochrome P450 17A1 inhibitors

Supplementary files

Article information

Article type
Communication
Submitted
28 Oct 2016
Accepted
16 Feb 2017
First published
28 Feb 2017

Chem. Commun., 2017,53, 3118-3121

Structure-based optimisation of non-steroidal cytochrome P450 17A1 inhibitors

M. Larsen, C. H. Hansen, T. B. Rasmussen, J. Islin, B. Styrishave, L. Olsen and F. S. Jørgensen, Chem. Commun., 2017, 53, 3118 DOI: 10.1039/C6CC08680B

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