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

โœ Scribed by William H Pearson; Luyi Guo


Publisher
Elsevier Science
Year
2001
Tongue
French
Weight
98 KB
Volume
42
Category
Article
ISSN
0040-4039

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โœฆ Synopsis


Swainsonine (3), an inhibitor of Golgi a-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.


๐Ÿ“œ SIMILAR VOLUMES


Synthesis and mannosidase inhibitory act
โœ William H Pearson; Erik J Hembre ๐Ÿ“‚ Article ๐Ÿ“… 2001 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 98 KB

Swainsonine (1), an inhibitor of the important glycoprotein-processing enzyme Golgi a-mannosidase II, is a clinical candidate for cancer treatment. Analogs bearing substituents at C-6 and C-7 have been prepared and evaluated as inhibitors of a-mannosidase (jack bean), a closely related enzyme.

Synthesis of the novel mannosidase inhib
โœ Erik J. Hembre; William H. Pearson ๐Ÿ“‚ Article ๐Ÿ“… 1997 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 805 KB

Swainsonine ( ) is an important mannosidase inhibitor that has been examined clinically as an anticancer drug. The preparation of analogs of swainsonine bearing a hydroxymethyl group at C(3), i.e., (3R)-3-(hydroxymethyl)swainsonine [( ), (3R)-HMS] and (3S)-3-(hydroxymethyl)swainsonine [( ), (3S)-HMS

Synthesis and ฮฑ-Mannosidase Inhibitory A
โœ Seiichiro Ogawa; Takayuki Morikawa ๐Ÿ“‚ Article ๐Ÿ“… 2000 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 313 KB ๐Ÿ‘ 1 views

Three deoxy derivatives 2-4 of the ฮฑ-mannosidase inhibitor mannostatin A (1) were synthesized, and their inhibition of Jack bean ฮฑ-mannosidase was evaluated in order to elucidate the roles of each of the three hydroxyl groups of the inhibitor. The 1-and 2-deoxy derivatives 2 and 3 retained some