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Updated: Jul 10, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Highly potent, water soluble benzimidazole antagonist for activated alpha 4 beta 1 integrin
Richard D Carpenter1, Mirela Andrei, Edmond Y Lau
1Department of Chemistry, University of California, Davis, Davis, CA 95616, USA.
Abstract:
The cell surface receptor alpha 4 beta 1 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.
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