| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10593210 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
A series of γ-lactam prostaglandin E1 analogs bearing a 16-phenyl moiety in the Ï-chain and aryl moiety in the α-chain were synthesized and biologically evaluated. Among the tested compounds, γ-lactam PGE analog 3 designed as a structural hybrid of 1 and 2 was discovered as the most optimized EP2/EP4 dual agonist with excellent subtype-selectivity (Ki values: mEP2 = 9.3 nM, mEP4 = 0.41 nM). A structure-activity relationship study is presented.
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Authors
Tohru Kambe, Toru Maruyama, Masayuki Nakano, Yoshihiko Nakai, Tadahiro Yoshida, Naoki Matsunaga, Hiroji Oida, Akira Konaka, Takayuki Maruyama, Hisao Nakai, Masaaki Toda,