Anisomycin derivatives and anticancer agents, antifungal agents

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D20712, C12P 1710, C12N 120, C12R 1465

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054630789

ABSTRACT:
Anisomycin derivatives represented by the following formula: ##STR1## and salts thereof, wherein R is hydrogen or an acyl group of 1-18 carbon atoms, and X is either a carbamoyl group represented by the formula --CONR.sup.1 R.sup.2 or an alkyl group represented by the formula --CH.sub.2 R.sup.3 in which R.sup.1 and R.sup.2 are each hydrogen, a linear or cyclic alkyl group of 1-6 carbon atoms which may have a substituent or a phenyl group which may have a substituent, and R.sup.3 is hydrogen, an alkyl group of 1-6 carbon atoms or an alkoxy group of 1-6 carbon atoms which may have a substituent, have improved stability in blood or plasma and are useful as anticancer agents, antifungal agents and antiprotozoan agents.

REFERENCES:
The Journal of Organic Chemistry, vol. 51, No. 7, Apr. 4, 1986, Hideo Iida, et al., "Highly Selective Total Synthesis of Enantiomerically Pure (-)-Anisomycin", pp. 1069-1073.
Chemical Abstracts, vol. 107, No. 25, Dec. 21, 1987, AN 236368e, JP-A-6 289 659.
Helvetica Chimica Acta, vol. 53, No. 4, 1970, I. Felner, et al., "Totalsynthese Des Antibioticums Anisomycin", pp. 754-763.
The Journal of Organic Chemistry, vol. 57, No. 4, Feb. 14, 1992, Roberto Ballini, et al., "A Nitrone-Based Approach to the Enantioselective Total Synthesis of (-)-Anisomycin", pp. 1316-1318.
The Journal of Organic Chemistry, vol. 53, No. 20, Sep. 30, 1988, Hans H. Baer, et al., "Stereospecific Synthesis of (-)-Anisomycin from D-Galactose", pp. 4786-4789.

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