Design, synthesis, and biological evaluation of novel potent and selective αvβ3/αvβ5 integrin dual inhibitors with improved bioavailability. Selection of the molecular …

…, B Anaclerio, L Lafrance, T Lu, T Markotan…

文献索引：Marugan, Juan Jose; Manthey, Carl; Anaclerio, Beth; Lafrance, Lou; Lu, Tianbao; Markotan, Tom; Leonard, Kristi A.; Crysler, Carl; Eisennagel, Stephen; Dasgupta, Malini; Tomczuk, Bruce Journal of Medicinal Chemistry, 2005 , vol. 48, # 4 p. 926 - 934

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被引用次数: 85

摘要

A novel series of potent and selective αvβ3/αvβ5 dual inhibitors was designed, synthesized, and evaluated against several integrins. These compounds were synthesized through a Mitsunobu reaction between the guanidinium mimetics and the corresponding central templates. Guanidinium mimetics with enhaced rigidity (ie,(2-pyridylamino) propoxy versus the 2-(6-methylamino-2-pyridyl) ethoxy) led to improved activity toward αvβ3. Exemplary ...