Development of flavonoid-based inverse agonists of the key signaling receptor US28 of human cytomegalovirus

…, MT Nguyen, N Tschammer, N Ocampo…

文献索引：Kralj, Ana; Nguyen, Mai-Thao; Tschammer, Nuska; Ocampo, Nicolette; Gesiotto, Quinto; Heinrich, Markus R.; Phanstiel, Otto Journal of Medicinal Chemistry, 2013 , vol. 56, # 12 p. 5019 - 5032

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被引用次数: 13

摘要

A series of 31 chalcone-and flavonoid-based derivatives were synthesized in good overall yields and screened for their inverse agonist activity on the US28 receptor of human cytomegalovirus (HCMV). With one exception (eg, 2-(5-bromo-2-methoxyphenyl)-3-hydroxy- 4 H-chromen-4-one), halogen-substituted flavonoids were typically more potent inverse agonists than their related hydro derivatives. While toxicity could be used to partially ...