Procaspase-activating compounds and compositions

摘要

The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.

主权项

1. A compound that directly activates procaspase-3 upon contacting procaspase-3, wherein the compound is a novel compound of Formula I:wherein
R1 is a substituted (aryl)methylene, or (aryl)methine wherein the methine carbon is optionally substituted with phenyl; n is 2; each R2 is methyl, ethyl or t-butyl or two R2 groups form an ortho-fused benzo group; and wherein R1 is substituted (aryl)methylene, the (aryl)methylene substitution comprises one or more nitro, sulfonamide, azidomethylene, phenoxy, phenyl, trifluoromethyl, trifluoromethoxy, phenylsulfonylmethylene, benzoyl, or a combination thereof; or a pharmaceutically acceptable salt or solvate thereof.