The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Synthesis and Protein Tyrosine Phosphatase Inhibitory Activity of Dephostatin Analogs
TAKUMI WATANABETOMIO TAKEUCHIMASAMI OTSUKASHIN-ICHIRO TANAKAKAZUO UMEZAWA
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JOURNAL FREE ACCESS

1995 Volume 48 Issue 12 Pages 1460-1466

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Abstract

We have synthesized derivatives of dephostatin, a protein tyrosine phosphatase (PTPase) inhibitor, to study the structure-activity relationships of this inhibitor. Inactive analogs revealed some insight into structural requirements for PTPase inhibitory activity of dephostatin. Both a nitroso group and phenolic hydroxyl groups were found to be essential for the inhibitory activity. Among the dephostatin derivatives synthesized, one of the regioisomers of dephostatin showed PTPase inhibitory activity equivalent to that of dephostatin, and also had increased stability.

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© Japan Antibiotics Research Association
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