Conjugates of Oligomer of Hyaluronic Acid or of a Salt Thereof, Method of Preparation Thereof and Use Thereof

摘要

The invention relates to conjugates of hyaluronic acid oligomer according to the general formulae I, II III or IV, or a salt thereof, the method of preparation thereof and use thereof, where the oligomer is bonded to the respective substrate by its ending anomeric center via a bi-functional amino linker by means of an amino or imino bond. This type of conjugates allows releasing oligomers in their native form. The prepared systems exhibited an enhanced biological activity against selected lines of cancer cells.;

主权项

1. A conjugate of an oligomer of hyaluronic acid or a salt thereof according to any of the general formulae I, II, III or IV, where R3 is COOR6 or CH2OH, R4 is OH or NHCOCH3, R6 is H+ or is selected from the group comprising any of alkali metal ions or alkaline earth metals, preferably Na+, K+, Mg2+ or Li+; R5 is selected from the group comprising C1-C30 alkyl, C1-C30 alkylaryl, or C1-C30 alkylheteroaryl optionally comprising one or more identical or different heteroatoms selected from the group comprising N, O, S; X is O or an NH group; in case that R3 is COOR6, R4 is OH, R1 is H, R2 is a hyaluronic acid oligomer residue; in case that R3 is CH2OH, R4 is NHCOCH3, R2 is OH, R1 is a hyaluronic acid oligomer residue; substrate is a polysaccharide.