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Title 

Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-γ-lactones as protein kinase C ligands and antitumor agents

Authors 

J H KangY KimS H WonSong Kyu ParkCahng Woo LeeHwan Mook KimN E LewinN A PerryL V PearceD J LundbergR J SurawskiP M BlumbergJ Lee

Publisher 

Elsevier

Issue Date 

2010

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 3, pp. 1008-1012

Keywords 

Antitumor activityDAG-lactoneDiacylglycerolProtein kinase C

Abstract 

A series of DAG-lactones with polar 3-alkylidene substituents have been investigated as PKC-α ligands and antitumor agents. Extensive analysis of structure-activity relationships for the 3-alkylidene chain revealed that polar groups such as ether, hydroxyl, aldehyde, ester, acyloxy, and amido were tolerated with similar binding affinities and reduced lipophilicities compared to the corresponding unsubstituted alkylidene chain. Among the derivatives, compounds 5, 6 and 8 with an ether type of side chain showed high binding affinities in range of Ki = 3-5 nM and excellent antitumor profiles, particularly against the colo205 colon cancer and the K562 leukemia cell lines.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2009.12.058

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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