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NOVEL APOPTOGENIC AGENTS FOR THE TREATMENT OF CHEMORESISTANT CANCERS |
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Principal Investigator: G. FOURNET
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TECHNICAL DESCRIPTION
This invention describes a novel family of therapeutic agents that induce apoptosis in cancer cells over-expressing the bcl2 gene. These compounds irreversibly inhibit the enzyme aldehyde dehydrogenase (ALDH), which catalyzes the oxidation of methional (a strong endogenous apoptogen) to the methylthio propionic acid (non-apoptogenic).They are thiolester derivatives of 4-amino 4-methyl 2-pentyne 1-al, an ALDH1 inhibitor. The technology also involves a method for preparing amino thiolesters in good yields.
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