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https://doi.org/10.1021/ml200067t
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 CDK2 kinase inhibitor MNK 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. 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 | URI: | http://scholarbank.nus.edu.sg/handle/10635/105945 | ISSN: | 19485875 | DOI: | 10.1021/ml200067t |
Appears in Collections: | Staff Publications |
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