| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369353 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenine moiety. The introduction of the amino group resulted in not only improved water solubility but also enhanced TLR7 agonistic activity. In particular compound 20 (DSR-6434) indicated an optimal balance between the agonistic potency and high water solubility. It also demonstrated a strong antitumor effect in vivo by intravenous administration in a tumor bearing mice model.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tomoaki Nakamura, Hiroki Wada, Hirotaka Kurebayashi, Tom McInally, Roger Bonnert, Yoshiaki Isobe,