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 language | English (US) |
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Pages (from-to) | 5863-5867 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 50 |
Issue number | 23 |
DOIs | |
State | Published - Nov 15 2007 |
ASJC Scopus subject areas
- Organic Chemistry