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Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors by B.A. Salameh; A. Sundin; H. Leffler; U.J. Nilsson is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Derivatives of N-acetyllactosamine carrying structurally diverse thioureido groups at galactose C3 were prepared from a C3'-azido N-acetyllactosamine derivative in a three-step reaction sequence involving azide reduction and isothiocyanate formation by thiophosgene treatment of the C3-amine, followed by reaction of the isothiocyanate with a panel of amines. Evaluation of the N-acetyllactosamine thioureas as inhibitors against galectins-1, 3, 7, 8N (N-terminal domain), and 9N (N-terminal domain) revealed thiourea-mediated affinity enhancements for galectins-1, 3, 7, and 9N. In particular, good inhibitors were discovered against galectin-7 and 9N (K(d) 23 and 47 microM, respectively, for a 3-pyridylmethylthiourea derivative), which represents more than an order of magnitude affinity enhancement over the parent natural N-acetyllactosamine.

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Author

B.A. Salameh; A. Sundin; H. Leffler; U.J. Nilsson

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2006

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)