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Title: Exploring aigialomycin D and its analogues as protein kinase inhibitors for cancer targets
Authors: Xu, J.
Chen, A.
Go, M.-L. 
Nacro, K.
Liu, B.
Chai, C.L.L. 
Keywords: Aigialomycin D
kinase inhibitor
resorcylic acid lactone
Issue Date: 8-Sep-2011
Citation: Xu, J., Chen, A., Go, M.-L., Nacro, K., Liu, B., Chai, C.L.L. (2011-09-08). Exploring aigialomycin D and its analogues as protein kinase inhibitors for cancer targets. ACS Medicinal Chemistry Letters 2 (9) : 662-666. ScholarBank@NUS Repository.
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 IC 50 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 (IC 50 = 0.45 μM), and preliminary structure-activity relationship studies have been carried out to identify the essential functional groups for activity. © 2011 American Chemical Society.
Source Title: ACS Medicinal Chemistry Letters
ISSN: 19485875
DOI: 10.1021/ml200067t
Appears in Collections:Staff Publications

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