Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Jane Wang; David Limburg; Jeff Carter; Gabriel Mbalaviele; James Gierse; Michael Vazquez

doi:10.1016/j.bmcl.2010.01.060

Selective inducible microsomal prostaglandin E₂ synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Jane Wang
, David Limburg
, Jeff Carter
, Gabriel Mbalaviele
, James Gierse
, Michael Vazquez

Research output: Contribution to journal › Article › peer-review

64 Scopus citations

Abstract

Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE₂ inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF_1α.

Original language	English
Pages (from-to)	1604-1609
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2010.01.060
State	Published - Mar 1 2010

Access to Document

10.1016/j.bmcl.2010.01.060

Cite this

@article{a9e39d35870b4206bd23c7ea1ef44c90,

title = "Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template",

abstract = "Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF1α.",

author = "Jane Wang and David Limburg and Jeff Carter and Gabriel Mbalaviele and James Gierse and Michael Vazquez",

year = "2010",

month = mar,

day = "1",

doi = "10.1016/j.bmcl.2010.01.060",

language = "English",

volume = "20",

pages = "1604--1609",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

number = "5",

}

TY - JOUR

T1 - Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

AU - Wang, Jane

AU - Limburg, David

AU - Carter, Jeff

AU - Mbalaviele, Gabriel

AU - Gierse, James

AU - Vazquez, Michael

PY - 2010/3/1

Y1 - 2010/3/1

N2 - Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF1α.

AB - Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF1α.

UR - https://www.scopus.com/pages/publications/76649142022

U2 - 10.1016/j.bmcl.2010.01.060

DO - 10.1016/j.bmcl.2010.01.060

M3 - Article

C2 - 20144869

AN - SCOPUS:76649142022

SN - 0960-894X

VL - 20

SP - 1604

EP - 1609

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Selective inducible microsomal prostaglandin E₂ synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Abstract

Access to Document

Other files and links

Fingerprint

Cite this