Synthesis and mannosidase inhibitory activity of 3-benzyloxymethyl analogs of swainsonine

Swainsonine ( 3 ), an inhibitor of Golgi α-mannosidase II, is a clinical candidate for cancer treatment. In order to avoid potential problems arising from its co-inhibition of lysosomal mannosidases, we have synthesized 3-benzyloxymethyl analogs of swainsonine ( 17 and 18 ). Initial screening of the...

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Bibliographic Details
Published inTetrahedron letters Vol. 42; no. 47; pp. 8267 - 8271
Main Authors Pearson, William H, Guo, Luyi
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 19.11.2001
Elsevier
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
ADVANCED MALIGNANCIES
SPECIFICITY
BIOSYNTHESIS
PURIFICATION
LYSOSOMAL ALPHA-MANNOSIDASE
RETAINING GLYCOSIDASES
GLYCOSYLATION
GLYCOSIDASE INHIBITORS
EXPRESSION
CHEMOTHERAPY
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Summary:Swainsonine ( 3 ), an inhibitor of Golgi α-mannosidase II, is a clinical candidate for cancer treatment. In order to avoid potential problems arising from its co-inhibition of lysosomal mannosidases, we have synthesized 3-benzyloxymethyl analogs of swainsonine ( 17 and 18 ). Initial screening of these new compounds is reported. Graphic
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(01)01777-4