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

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

doi:10.1039/C6CC08680B

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

Morten Larsen, Cecilie Hurup Hansen, Tobias B. Rasmussen, Bjarne Styrishave, Lars Olsen, Flemming Steen Jørgensen

3 Citations (Scopus)

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.

Original language	English
Article number	3118
Journal	Chemical Communications
Volume	53
Issue number	3118
Number of pages	4
ISSN	1359-7345
DOIs	https://doi.org/10.1039/C6CC08680B
Publication status	Published - 28 Feb 2017

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10.1039/C6CC08680BLicence: Unspecified

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title = "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.",

author = "Morten Larsen and Hansen, {Cecilie Hurup} and Rasmussen, {Tobias B.} and Bjarne Styrishave and Lars Olsen and J{\o}rgensen, {Flemming Steen}",

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T1 - Structure-based optimisation of non-steroidal cytochrome P450 17A1 inhibitors

AU - Larsen, Morten

AU - Hansen, Cecilie Hurup

AU - Rasmussen, Tobias B.

AU - Styrishave, Bjarne

AU - Olsen, Lars

AU - Jørgensen, Flemming Steen

PY - 2017/2/28

Y1 - 2017/2/28

N2 - 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.

AB - 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.

U2 - 10.1039/C6CC08680B

DO - 10.1039/C6CC08680B

M3 - Journal article

SN - 1359-7345

VL - 53

JO - Chemical Communications

JF - Chemical Communications

IS - 3118

M1 - 3118

ER -

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

Abstract

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