7-O-(2,6-Dideoxy-.alpha.-L-lyxo-hexopyranosyl)-daunomycinone, de

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 17A, A61K 3171, C07H 1524

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active

042017734

ABSTRACT:
A series of compounds showing high antileukemic activity against P388 murine leukemia and increased aqueous solubility due to substitution of --OH for the known --NH.sub.2 at the 3' position of the hexopyranose sugar, i.e., daunosamine.
These compounds are coupled products of aglycon selected from daunomycinone, desmethoxy daunomycinone, adriamycinone and carminomycinone. These compounds are coupled at the 0-7 position of the aglycon with an .alpha.-L-lyxo hexopyranose sugar, which sugar isomer particularly sustains or potentiates the biological activity of the coupled compound as well as ameliorates the dose related cardiotoxicity of the parent and known compounds set out below: ##STR1##

REFERENCES:
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patent: 4046878 (1977-09-01), Patelli et al.
patent: 4058519 (1977-11-01), Arcamone et al.
patent: 4067968 (1978-01-01), Lazzari et al.
patent: 4067969 (1978-01-01), Penco et al.
Fuchs et al., "Carbohydrate Research", vol. 57, 1977, C36-C39.
Cheung et al., "Carbohydrate Research", vol. 58, 1977, pp. 139-151.

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