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Bioorg Med Chem Lett. 2011 Jan 1;21(1):307-10. doi: 10.1016/j.bmcl.2010.11.014. Epub 2010 Nov 5.

Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.

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1
Sunesis Pharmaceuticals, Inc, 395 Oyster Point Blvd, Suite 400, South San Francisco, CA 94080, USA. mzhong@presidiopharma.com

Abstract

This letter describes the structure-activity relationship (SAR) of the 'right-wing' α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists. Novel (S)-substituted heteroaryl-bearing α-amino acids have been identified as replacements of the 'right-wing' (S)-2,3-diaminopropanoic acid (DAP) moiety. Improvement of potency in the Hut-78 assay in the presence of 10% human serum has also been achieved.

PMID:
21109434
DOI:
10.1016/j.bmcl.2010.11.014
[Indexed for MEDLINE]
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