The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
CHEMICAL MODIFICATION OF THE ANTITUMOR ANTIBIOTIC GLIDOBACTIN
MASAHISA OKAKEI-ICHI NUMATAYUJI NISHIYAMAHIDEO KAMEIMASATAKA KONISHITOSHIKAZU OKIHIROSHI KAWAGUCHI
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1988 Volume 41 Issue 12 Pages 1812-1822

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Abstract

A variety of glidobactin analogs modified at the fatty acid, L-threonine and nucleus moieties of the molecule were synthesized and their structure-activity relationships examined. The antitumor and antifungal activity was greatly influenced by modification of the fatty acid glidobactin, with the dodecanoyl and tetradecanoyl analogs exhibiting better antitumor activity than the parent antibiotics. Replacement of the L-threonine with other amino acids greatly reduced the activity and reduction of the double bond of the nucleus completely eliminated the biological activity of glidobactin.

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© Japan Antibiotics Research Association
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