Please use this identifier to cite or link to this item:
|Title:||Exploring aigialomycin D and its analogues as protein kinase inhibitors for cancer targets|
resorcylic acid lactone
|Source:||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|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Feb 14, 2018
WEB OF SCIENCETM
checked on Jan 22, 2018
checked on Feb 19, 2018
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.