C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
260/208.2
C07H 15/24 (2006.01) C07H 3/02 (2006.01) C07H 13/04 (2006.01) C07H 15/04 (2006.01) C07H 15/252 (2006.01)
Patent
CA 1141757
ABSTRACT OF THE DISCLOSURE A series of compounds showing high antileukemic activity against P388 murine leukemia and increased aqueous solubility due to substitution of -OH for the known -NH2 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: (1) R1=H; R2=OMe (2) R1=OH; R2=OMe Image (3) R1=H; R2=OH (4) R1=H; R2=H (5) R3=H or acetyl.
332489
Cheung Tak M.
Fuchs Ernst F.
Horton Derek
Sorenson Roderick J.
Weckerle Wolfgang F.
Smart & Biggar
United States Of America As Represented By The Secretary Of Comm
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