HIGH-MOLECULAR WEIGHT CONJUGATE OF PODOPHYLLOTOXINS Russian patent published in 2012 - IPC C08G81/00 C08G85/00 C08G65/32 A61K47/48 A61K47/34 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to anticancer agents containing a high-molecular weight conjugate of podophyllotoxins. Disclosed is an anticancer agent which contains a high-molecular weight conjugate of podophyllotoxins, having formula

,

where R1 denotes hydrogen or a (C1-C6)-alkyl group; R2 denotes a binding group; R3 denotes hydrogen or a (C1-C6)-acyl group; R4 denotes a residue of the hydroxyl group of podophyllotoxins; R5 is selected from (C1-C30)-alkoxy group, (C7-C30)-aralkyloxy group, (C1-C30)-alkylamino group, di-(C1-C30)-alkylamino group, an amino acid with a protected carboxyl group and -N(R6)CONH(R7), where each of R6 and R7, which can be identical or different, denotes a cyclic (C3-C6)-alkyl group or a (C1-C5)-alkyl group which is optionally substituted with a tertiary amine group; t = 5 - 11500; each of d, e, f, g, h, i and j is independently a whole number from 0 to 200, provided that d+e is a whole number from 1 to 200, and d+e+f+g+h+i+j is a whole number from 3 to 200 and that corresponding component units of polyaspartic acid are linked in any order.

EFFECT: disclosed anticancer agent is soluble in water and has high therapeutic activity.

4 cl, 2 dwg, 2 tbl, 3 ex