Mono-carbonyl curcumin analogues as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
Journal: Bioorganic & Medicinal Chemistry Letters
Published:
Abstract
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.
Authors
Han Lin, Guo-xin Hu, Jingjing Guo, Yufei Ge, Guang Liang, Qing-quan Lian, Yanhui Chu, Xiaohuan Yuan, Ping Huang, Ren-shan Ge