Search Results - "Yu, Chul H"
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Discovery of a potent and selective Aurora kinase inhibitor
Published in Bioorganic & medicinal chemistry (01-09-2008)“…The discovery of a novel series of Aurora kinase inhibitors is disclosed. This communication describes the discovery of a novel series of Aurora kinase…”
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2
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye
Published in ACS medicinal chemistry letters (08-03-2012)“…LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte…”
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3
2-Aminobenzimidazoles as potent Aurora kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…This Letter describes the discovery and key structure–activity relationship (SAR) of a series of 2-aminobenzimidazoles as potent Aurora kinase inhibitors…”
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4
Structure–activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…Structure–activity relationship (SAR) of the α-amino acid residue and identification of (S)-2,3-diaminopropanoic acid (DAP) replacements of potent…”
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Water-soluble prodrugs of an Aurora kinase inhibitor
Published in Bioorganic & medicinal chemistry letters (01-03-2009)“…In vitro and in vivo properties of prodrug derivatives of the Aurora kinase inhibitor SNS-314 are described. Compound 1 (SNS-314) is a potent and selective…”
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Synthesis and biological activity of selective pipecolic acid-based TNF-α converting enzyme (TACE) inhibitors
Published in Bioorganic & medicinal chemistry letters (20-05-2002)“…A series of novel, selective TNF-α converting enzyme inhibitors based on 4-hydroxy and 5-hydroxy pipecolate hydroxamic acid scaffolds is described. The potency…”
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7
Identification of nonpeptidic small-molecule inhibitors of interleukin-2
Published in Bioorganic & medicinal chemistry letters (15-02-2005)“…The identification, design, and synthesis of a series of novel sulfamide- and urea-based small-molecule antagonists of the protein–protein interaction…”
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Integrating Fragment Assembly and Biophysical Methods in the Chemical Advancement of Small-Molecule Antagonists of IL-2: An Approach for Inhibiting Protein−Protein Interactions
Published in Journal of medicinal chemistry (03-06-2004)“…Fragment assembly has shown promise for discovering small-molecule antagonists for difficult targets, including protein−protein interactions. Here, we describe…”
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Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists
Published in Bioorganic & medicinal chemistry letters (01-09-2010)“…The discovery of a novel series of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists is described. This…”
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10
Benzimidazolone p38 inhibitors
Published in Bioorganic & medicinal chemistry letters (23-02-2004)“…The synthesis and in vitro p38 alpha activity of a novel series of benzimidazolone inhibitors is described. The p38 alpha SAR is consistent with a mode of…”
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Synthesis and biological activity of piperazine-Based dual MMP-13 and TNF-α converting enzyme inhibitors
Published in Bioorganic & medicinal chemistry letters (06-10-2003)“…A series of novel MMP-13 and TNF-α converting enzyme inhibitors based on piperazine 2-hydroxamic acid scaffolds are described. The TACE, MMP-1 and MMP-13…”
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