TREATMENT OF HUMAN PROSTATE DISEASE WITH BETA-LAPACHONE DERIVATIVES

摘要

We have now discovered that unexpectedly compounds of formulae (I) or (II) can be used to selectively stimulate the death of mammalian prostate cells, including both epithelial cell and prostate cancer cells, and thus are useful in treating prostate diseases, wherein R and R1 are each independently selected from the group consisting of hydrogen, hydroxy, thio (SH), halogen, substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted aryl, and substituted and unsubstituted alkoxy, and salts thereof, wherein the dotted double bond between the ring carbons to which R and R1 are bonded represent an optional ring double bond. Preferred compounds of formula (I) include those in which at least one of the substituents R and R1 is hydrogen and/or at least one said substituents is allyl. Specifically preferred compounds include beta -lapachone (i.e., R and R1, both being hydrogen), allyl- beta -lapachone, particularly 3-allyl- beta -lapachone (i.e. R being allyl and R1 being hydrogen) and 3-bromo- beta -lapachone (i.e. R being bromo and R1 being hydrogen).