Highly potent, water soluble benzimidazole antagonist for activated α4β1 integrin

Richard D. Carpenter, Mirela Andrei, Edmond Y Lau, Felice C Lightstone, Ruiwu Liu, Kit Lam, Mark J. Kurth

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

The cell surface receptor α4β1 integrin, activated constitutively in lymphoma, can be targeted with the bisaryl urea peptidomimetic antagonist 1 (LLP2A). However, concerns on its preliminary pharmacokinetic (PK) profile provided an impetus to change the pharmacophore from a bisaryl urea to a 2-arylaminobenzimidazole moiety, resulting in improved solubility while maintaining picomolar potency [5 (KLCA4); IC50 = 305 pM]. With exceptional solubility, this finding has the potential for improving PK to help diagnose and treat lymphomas.

Original languageEnglish (US)
Pages (from-to)5863-5867
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number23
DOIs
StatePublished - Nov 15 2007

ASJC Scopus subject areas

  • Organic Chemistry

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