Abstract: This invention relates to macromolecular prodrugs having antitumor activity when activated by GSH, and methods for synthesizing and administering these to patients. More particularly, this invention relates to, inter alia, the synthesis and use of polyacrylamide carriers to target anticancer prodrugs to tumors, and to release active antitumor agents selectively in tumor cells. These active antitumor agents target the active site of the methylglyoxal-detoxifying enzyme glyoxalase I to thereby cause tumor regression.

Abstract: Compounds comprising two human GlxI inhibitors covalently linked via a chemical linker are provided, wherein each of said two human GlxI inhibitors, which may be the same or different, is an S-substituted glutathione or an S-substituted glutathione prodrug, wherein said GlxI inhibitors each have a ?-glutamyl amino group, wherein said chemical linker is covalently bound to each GlxI inhibitor via said ?-glutamyl amino group, and wherein said chemical linker has a length of at least 50 Angstroms. Monovalent irreversible inactivators of human GlxI are also provided. An antineoplastic composition is provided, which comprises a compound described above and a pharmaceutically acceptable carrier. In vitro and in vivo methods of preventing or inhibiting the growth and proliferation of neoplastic cells and/or tumors are also provided.

Abstract: Described herein are new enone derivatives and conjugates. Additionally, methods for synthesizing these new enones are also disclosed. These compounds can be employed in cancer therapy.

Abstract: The present invention provides a compound having the structure ##STR1## wherein S* is S.dbd.O or O.dbd.S.dbd.O; and wherein R.sub.1 is selected from the group consisting of (C.sub.1 -C.sub.9) alkyl, (C.sub.3 -C.sub.8) cycloalkyl, (C.sub.5 -C.sub.7) cycloalkenyl, and (C.sub.6 -C.sub.20) aryl substituted with halogen or (C.sub.1 -C.sub.18) alkyl; and wherein R.sub.2 is selected from the group consisting of alkyl, (C.sub.1 -C.sub.9) alkyl, (C.sub.3 -C.sub.8) cycloalkyl, (C.sub.5 -C.sub.7) cycloalkenyl, and (C.sub.6 -C.sub.20) aryl substituted with halogen or (C.sub.1 -C.sub.18) alkyl. Also provided are various methods of using the compositions of the present invention.