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|Title:||Exploring aigialomycin D and its analogues as protein kinase inhibitors for cancer targets|
resorcylic acid lactone
|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. https://doi.org/10.1021/ml200067t|
|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|
|Appears in Collections:||Staff Publications|
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