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

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Title
Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-γ-lactones as protein kinase C ligands and antitumor agents
Author(s)
J H Kang; Y Kim; S H Won; Song Kyu Park; Cahng Woo Lee; Hwan Mook Kim; N E Lewin; N A Perry; L V Pearce; D J Lundberg; R J Surawski; P M Blumberg; J Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 3, pp. 1008-1012
Publication Year
2010
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.
Keyword
Antitumor activityDAG-lactoneDiacylglycerolProtein kinase C
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2009.12.058
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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