The 2nd Affiliated Hospital & Institute of Reproductive Biomedicine, Wenzhou Medical College, Wenzhou 325000, China.
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4362-6. doi: 10.1016/j.bmcl.2013.05.080. Epub 2013 Jun 11.
A series of structurally novel mono-carbonyl curcumin analogues have been synthesized and biologically evaluated to test their inhibitory potencies and the structure-activity relationship (SAR) on human and rat 11β-hydroxysteroid dehydrogenase isoform (11β-HSD1) activities. 11β-HSD1 selective inhibitors have been discovered and compound A10 is discovered as a very potent with an IC50 value of 97 nM without inhibiting 11β-HSD2.
已经合成了一系列结构新颖的单羰基姜黄素类似物，并对其进行了生物评估，以测试它们对人和大鼠 11β-羟甾类脱氢酶同工酶（11β-HSD1）活性的抑制效力和构效关系（SAR）。已经发现了 11β-HSD1 的选择性抑制剂，并且发现化合物 A10 是一种非常有效的抑制剂，其 IC50 值为 97 nM，而不抑制 11β-HSD2。
