A new compound FR-68504, production thereof and use thereof.

摘要

57 The invention relates to a new compound, designated FR-68504. The compound has antitumor activities and is effective in the treatment of various tumors in both human beings and animals.

There is also provided a process for preparing FR-68504 compound which comprises culturing a FR-68504 producing strain belonging to the genus Amauroascus in a nutrient medium.

Pharmaceutical composition comprising FR-68504 as an active ingredient is also described.<!-- EPO <DP n="2"> -->

<UnorderedLists id="ula01" listStyle="none"><ListItem>f) UV absorption spectrum :
<UnorderedLists id="ula02" listStyle="none"><ListItem>End absorption (in H<Sub>2</Sub>0)</ListItem></UnorderedLists></ListItem><ListItem>g) IR absorption spectrum :
<UnorderedLists id="ula03" listStyle="none"><ListItem>Nujol: 3400, 3250, 1300, 1100, 1030, 950, max 850 cm-1</ListItem></UnorderedLists></ListItem><ListItem>h) <Sup>1</Sup>H NMR absorption spectrum : (D<Sub>2</Sub>0) δppm: 3.94-3.78 (4H, m), 3.57 (lH, dd, J=9.2 and 5.3Hz), 3.36-3.25 (2H, m), 3.01-2.88 (4H, m)</ListItem><ListItem>i) 13<Sub>C NMR</Sub> absorption spectrum : (D<Sub>2</Sub>0) δppm: 71.0 (d), 70.6 (d), 70.4 (d), 69.6 (d), 68.6 (d) , 55.1 (d), 53.5 (d) , 46.6 (t), 46.5 (t)</ListItem><ListItem>j) Solubility :
<UnorderedLists id="ula04" listStyle="none"><ListItem>Soluble : Water</ListItem><ListItem>Sparingly soluble : Methanol, ethanol, acetone</ListItem><ListItem>Insoluble : Ethyl acetate, chloroform</ListItem></UnorderedLists></ListItem><ListItem>k) Color reaction :
<UnorderedLists id="ula05" listStyle="none"><ListItem>Positive : Molish's reaction, reaction with cerium sulfate</ListItem><ListItem>Negative : Ninhydrin reaction, ferric chloride-potassium ferricyanide reaction, reaction with Dragendorff reagent or iodine vapor.</ListItem></UnorderedLists></ListItem><ListItem>1) Property of substance :
<UnorderedLists id="ula06" listStyle="none"><ListItem>Neutral substance</ListItem><ListItem>m) Thin layer chromatography (silica gel sheet) :<Image id="ia01" he="28" wi="141" file="IMGA0001.TIF" imgContent="table" imgFormat="TIFF" inline="no" /></ListItem></UnorderedLists></ListItem></UnorderedLists>

The FR-68504 can be prepared by culturing a FR-68504-producing strain belonging to the genus