Discovery and SAR of hydantoin TACE inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
We disclose inhibitors of TNF-{alpha} converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Crystal structures of inhibitors bound to TACE revealed monodentate coordination of the hydantoin to the zinc. SAR, X-ray, and modeling designs are described. To our knowledge, these are the first reported X-ray structures of TACE with a hydantoin zinc ligand.
- Research Organization:
- Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1002639
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (6) ; 03, 2010 Vol. 20; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
Similar Records
The discovery of novel tartrate-based TNF-[alpha] converting enzyme (TACE) inhibitors
5-Amino-pyrazoles as potent and selective p38[alpha] inhibitors
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors
Journal Article
·
Fri Sep 17 00:00:00 EDT 2010
· Bioorg. Med. Chem. Lett.
·
OSTI ID:1002634
5-Amino-pyrazoles as potent and selective p38[alpha] inhibitors
Journal Article
·
Mon Feb 06 23:00:00 EST 2012
· Bioorg. Med. Chem. Lett.
·
OSTI ID:1025635
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors
Journal Article
·
Fri Sep 12 00:00:00 EDT 2008
· J. Med. Chem.
·
OSTI ID:1007657