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
1
Wyeth Research, 401 N. Middletown Rd., Pearl River, NY 10965, USA
|
2
Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
|
3
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
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
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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Total citations:
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Citations from 2024:
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(8.89%)
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GOST
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Levin J. et al. Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates // Bioorganic and Medicinal Chemistry Letters. 2006. Vol. 16. No. 6. pp. 1605-1609.
GOST all authors (up to 50)
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Levin J., Chen J. M., Laakso L. M., Du M., Schmid J., Xu W., Cummons T., Xu J., JIN G., BARONE D., Skotnicki J. Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates // Bioorganic and Medicinal Chemistry Letters. 2006. Vol. 16. No. 6. pp. 1605-1609.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2005.12.020
UR - https://doi.org/10.1016/j.bmcl.2005.12.020
TI - Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Levin, J.
AU - Chen, J. M.
AU - Laakso, L M
AU - Du, Min
AU - Schmid, J
AU - Xu, Wei
AU - Cummons, T.
AU - Xu, Jianbin
AU - JIN, G.
AU - BARONE, D.
AU - Skotnicki, J.S.
PY - 2006
DA - 2006/03/01
PB - Elsevier
SP - 1605-1609
IS - 6
VL - 16
PMID - 16426848
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2006_Levin,
author = {J. Levin and J. M. Chen and L M Laakso and Min Du and J Schmid and Wei Xu and T. Cummons and Jianbin Xu and G. JIN and D. BARONE and J.S. Skotnicki},
title = {Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2006},
volume = {16},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2005.12.020},
number = {6},
pages = {1605--1609},
doi = {10.1016/j.bmcl.2005.12.020}
}
Cite this
MLA
Copy
Levin, J., et al. “Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.” Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 6, Mar. 2006, pp. 1605-1609. https://doi.org/10.1016/j.bmcl.2005.12.020.