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 Citationer (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.

Originalsprog	Engelsk
Artikelnummer	3118
Tidsskrift	Chemical Communications
Vol/bind	53
Udgave nummer	3118
Antal sider	4
ISSN	1359-7345
DOI	https://doi.org/10.1039/C6CC08680B
Status	Udgivet - 28 feb. 2017

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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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