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J Med Chem. 1992 Jul 24;35(15):2768-71.

Inhibition of collagenase by aranciamycin and aranciamycin derivatives.

Author information

1
Department of Organic Chemistry, Technical University of Denmark, Lyngby.

Abstract

Aranciamycin (1), an anthracycline antibiotic, was found to be an inhibitor of Clostridium histolyticum collagenase, with an IC50 = 3.7 x 10(-7) M. Elastase and trypsin were not inhibited at concentrations less than or equal to 10(-5) M. A number of aranciamycin derivatives 2-13 were prepared and tested for collagenase inhibition. While loss of activity was found for derivatives modified in the sugar ring or rings B and D of the aglycone, increased potency was found when the tertiary alcohol at C-9 was esterified. All compounds 1-13 were found to inhibit DNA synthesis of Yoshida sarcoma tumor cells.

PMID:
1322986
DOI:
10.1021/jm00093a008
[Indexed for MEDLINE]

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