[EN] 7-0-(2,6-DIDEOXY-A-L-LYXO-HEXOPYRANOSYL)-DESMETHOXYDAUNOMYCINONE,ADRIAMYCINONE,AND CARMINOMYCINONE
申请人:——
公开号:WO1980000305A1
公开(公告)日:1980-03-06
(EN) A series of compounds showing high antileukemic activity against P388 murine leukemia and increased aqueous solubility due to substitution of -0H for the known -NH2 at the 3" position of the hexopyranose sugar, i.e., daunosamine. These compounds are coupled products of aglycon selected from desmthoxy 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: (FR) Les composes ont une grande activite antileucemique sur les leucemies murine P 388 et une meilleure solubilite aqueuse due a la substitution du groupe NH2 par un groupe OH en position 3" de l"exopyranose, c"est-a-dire la daunosamine. Ces composes sont des produits de liaison de l"aglycone de la desmethoxy daunomycinone, de l"ordriamycinone et de la carminomycinone. Ces composes sont lies en position 0-7 de l"aglycone avec un (Alpha)-L-lyxo hexopyranose, l"isomere de ce glucide soutenant en particulier ou renforce l"activite biologique de compose de liaison tout en diminuant la cardiotoxicite des composes connus. Ces composes repondent a formule: