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) |
|---|---|
| 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 |
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ASJC Scopus subject areas
- Organic Chemistry
Cite this
Highly potent, water soluble benzimidazole antagonist for activated α4β1 integrin. / Carpenter, Richard D.; Andrei, Mirela; Lau, Edmond Y; Lightstone, Felice C; Liu, Ruiwu; Lam, Kit; Kurth, Mark J.
In: Journal of Medicinal Chemistry, Vol. 50, No. 23, 15.11.2007, p. 5863-5867.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Highly potent, water soluble benzimidazole antagonist for activated α4β1 integrin
AU - Carpenter, Richard D.
AU - Andrei, Mirela
AU - Lau, Edmond Y
AU - Lightstone, Felice C
AU - Liu, Ruiwu
AU - Lam, Kit
AU - Kurth, Mark J.
PY - 2007/11/15
Y1 - 2007/11/15
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=36148929378&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=36148929378&partnerID=8YFLogxK
U2 - 10.1021/jm070790o
DO - 10.1021/jm070790o
M3 - Article
C2 - 17948981
AN - SCOPUS:36148929378
VL - 50
SP - 5863
EP - 5867
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 23
ER -