New glycolipid inhibitors of Myt1 kinase

A crude extract of a marine alga showed activity against the enzyme Myt1 kinase. Bioassay-directed fractionation led to the isolation of two bioactive glycoglycerolipids. Lipid 1 was identified as sn-1,2-dipalmityl-3-( N-palmityl-6-deoxy-6-amino-α- d-glucosyl) glycerol and lipid 2 as sn-1-palmityl-2...

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Bibliographic Details
Published in:Tetrahedron 2005-01, Vol.61 (4), p.883-887
Main Authors: Zhou, Bing-Nan, Tang, Shoubin, Johnson, Randall K., Mattern, Michael P., Lazo, John S., Sharlow, Elizabeth R., Harich, Kim, Kingston, David G.I.
Format: Article
Language:English
Subjects:
Glycolipid
Marine
Myt1 kinase
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Summary:A crude extract of a marine alga showed activity against the enzyme Myt1 kinase. Bioassay-directed fractionation led to the isolation of two bioactive glycoglycerolipids. Lipid 1 was identified as sn-1,2-dipalmityl-3-( N-palmityl-6-deoxy-6-amino-α- d-glucosyl) glycerol and lipid 2 as sn-1-palmityl-2-myristyl-3-( N-stearyl-6-deoxy-6-aminoglucosyl)glycerol. Compounds 1 and 2 had IC 50 values of 0.12 and 0.43 μg/mL, respectively, in the Myt1 kinase inhibitory bioassay, and were inactive against Akt and Chk1 kinases. Bioassay-directed fractionation of a marine algal species using a bioassay for inhibitors of the enzyme Myt1 kinase yielded the novel glycoglycerolipids 1 and 2 as the major bioactive constituents. The structures of 1 and 2 were assigned by NMR spectra together with chemical and enzymatic degradations and by analyses of mass spectroscopic data.
ISSN:0040-4020
1464-5416
DOI:10.1016/j.tet.2004.11.013