Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors
Our previous studies have demonstrated that osthole, a Chinese herbal compound, could be incorporated into the hydroxycinnamide scaffold of LBH-589, a potent HDAC inhibitor, as an effective hydrophobic cap; the resulting compounds showed significant poten
Discovery of novel osthole derivatives as potential anti-breast cancer treatment
Osthole, an ingredient of Traditional Chinese Medicine (TCM) from natural product Cnidium monnieri (L.) Cusson, was used as a lead compound for structural modification. A series of osthole derivatives bearing aryl substituents at 3-position of coumarin, h
You, Lisha,An, Rui,Wang, Xinhong,Li, Yimin
supporting information; experimental part
p. 7426 - 7428
(2011/02/23)
Identification and structure-activity relationship studies of osthol, a cytotoxic principle from Cnidium monnieri
Osthol (1) was isolated from the fruit of Cnidium monnieri as a cytotoxic principle. Its structure-activity relationship study reveals that the 3,4-olefinic bond is essential for its cytotoxic activity, and the prenyl (C5) unit attached at the 8 position enhances the cytotoxicity. Analogues 7 and 8 that have a longer alkoxy unit at the 7 position showed ten times higher cytotoxicity than 1.