Hybrid antitumor compounds containing a cyclic enediyne and a DNA- binder

摘要

The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I) P PD--(OCH.sub.2).sub.m --O--(CH.sub.2).sub.n --Ar--Y--CONH-- B(I) PPwherein D is a cyclic enediyne; B is a residue capable of binding to the minor groove of DNA; n is 0 and m is 1, is or n is 1 and m is 0 or 1; Ar is an aromatic residue selected from the group consisting of phenyl, naphthyl, pyridyl, quinolinyl and indolyl; and Y is a direct bond, --CH.sub.2 -- or --CH═CH--; or a pharmaceutically acceptable salt thereof.