作为酪氨酸酶抑制剂的羟基取代2-苯基萘的合成
Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase.
作者信息
Song Suhee, Lee Hyojin, Jin Youngeup, Ha Young Mi, Bae Sungjin, Chung Hae Young, Suh Hongsuk
机构信息
Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University, Busan 609-735, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2007 Jan 15;17(2):461-4. doi: 10.1016/j.bmcl.2006.10.025. Epub 2006 Oct 12.
Oxyresveratrol and resveratrol, with hydroxy substituted trans-stilbene structure, exert potent inhibitory effects on cyclooxygenase, rat liver mitochondrial ATPase activity, and tyrosinase. As the isosteres of oxyresveratrol, a new family of hydroxyl substituted phenyl-naphthalenes were synthesized to show excellent inhibition of mushroom tyrosinase. Compound 10, which is isostere of resveratrol, showed IC50 value of 16.52 microM in mushroom tyrosinase activity. As compared to this, the reference compound, resveratrol, showed IC50 value of 55.61 microM. Compound 4, which is isostere of oxyresveratrol, showed IC50 value of 0.49 microM. Among the other three derivatives, compound 13 showed IC50 value of 0.034 microM.
氧化白藜芦醇和白藜芦醇具有羟基取代的反式芪结构，对环氧化酶、大鼠肝脏线粒体ATP酶活性和酪氨酸酶具有强大的抑制作用。作为氧化白藜芦醇的电子等排体，合成了一个新的羟基取代苯基萘家族，以显示出对蘑菇酪氨酸酶的优异抑制作用。化合物10是白藜芦醇的电子等排体，在蘑菇酪氨酸酶活性中显示出16.52微摩尔的IC50值。与此相比，参考化合物白藜芦醇的IC50值为55.61微摩尔。化合物4是氧化白藜芦醇的电子等排体，IC50值为0.49微摩尔。在其他三种衍生物中，化合物13的IC50值为0.034微摩尔。
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