Bioorganic and Medicinal Chemistry Letters, volume 16, issue 6, pages 1605-1609

Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates

J. Levin ¹

J. M. Chen ¹

L M Laakso ¹

Min Du ¹

J Schmid ¹

Wei Xu ²

T. Cummons ³

Jianbin Xu ¹

G. JIN ¹

D. BARONE ⁴

J.S. Skotnicki ¹

Show full list: 11 authors

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Wyeth Research, 401 N. Middletown Rd., Pearl River, NY 10965, USA |

Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA |

Wyeth Research, PO Box CN-8000, Princeton, NJ 08543, USA |

⁴

Amgen, Seattle, WA 98101, USA |

Publication type: Journal Article

Publication date: 2006-03-01

Elsevier

Journal: Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

SJR: 0.508

CiteScore: 5.7

Impact factor: 2.5

ISSN: 0960894X, 14643405

DOI: 10.1016/j.bmcl.2005.12.020

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PubMed ID: 16426848

Organic Chemistry

Drug Discovery

Biochemistry

Molecular Biology

Pharmaceutical Science

Clinical Biochemistry

Molecular Medicine

Abstract

A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1' groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-alpha production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.

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Publisher

Elsevier

Journal

Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

SJR

0.508

CiteScore

5.7

Impact factor

2.5

ISSN

0960894X (Print)

14643405 (Electronic)

Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates

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