Basic Information
ID: ALA2010797
Journal: ACS Med Chem Lett
Title: Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
Authors: Xu J, Chen A, Go ML, Nacro K, Liu B, Chai CL.
Abstract: The natural product aigialomycin D (1) is a member of the resorcylic acid lactone (RAL) family possessing protein kinase inhibitory activities. This paper describes the synthesis of aigialomycin D and a series of its analogues and their activity for the inhibition of protein kinases related to cancer pathways. A preliminary study of these compounds in the inhibition of CDK2/cyclin A kinase has found that aigialomycin D and analogues 11 and 23 are moderate CDK2/cyclin A inhibitors with IC50 values of ca. 20 μM. Kinase profiling of aigialomycin D against a panel of kinases has led to the identification of MNK2 as a promising target (IC50 = 0.45 μM), and preliminary structure-activity relationship studies have been carried out to identify the essential functional groups for activity.
CiteXplore: 24900361
DOI: 10.1021/ml200067t
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets