University System of Maryland

Cornell University

Diana S Hamilton

Donald J Creighton

Bruce Ganem

Malcolm J Kavarana

Zhebo Ding

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.

Enone cancer therapeutics

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.

Competitive inhibitors of glyoxalase I and method of generating such

A compound of the formula ##STR1## with R being hydrogen, alkyl, cycloalkyl or aryl, which may be substituted with halogen or alkyl, and R' and R.sup.a being hydroxyl, or --O-alkyl, pharmaceutically acceptable salts thereof; or mixtures thereof. An anti-neoplastic composition comprises the 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 comprise contacting the cells with or administering to a subject an anti-growth and proliferation effective amount of the compound described above.

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Catonsville, MD, United States of America

Diana S Hamilton