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

Morten Larsen; Cecilie H. Hansen; Tobias B. Rasmussen; Julie Islin; Bjarne Styrishave; Lars Olsen; Flemming Steen Jørgensen

doi:10.1039/C6CC08680B

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

Morten Larsen,^a Cecilie H. Hansen,^b Tobias B. Rasmussen,

^b Julie Islin,^b Bjarne Styrishave,^b Lars Olsen

^a and Flemming Steen Jørgensen

*^a

Author affiliations

* Corresponding authors

^a Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, DK-2100 Copenhagen, Denmark
E-mail: fsj@sund.ku.dk

^b Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark

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.

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Article information

DOI: https://doi.org/10.1039/C6CC08680B
Article type: Communication
Submitted: 28 Oct 2016
Accepted: 16 Feb 2017
First published: 28 Feb 2017

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

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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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Chemical Communications

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

Abstract

Supplementary files

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

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