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This invention relates to novel therapeutics directed against castrate resistant prostate cancer (CRPC). Twenty percent of all prostate cancers develop into CRPC which is uniformly fatal. CRPC often arises because tumors synthesize androgens independent of the testes.
The Penning Lab has previously determined that AKR1C3 is the primary enzyme responsible for the production of testosterone in the prostate. This invention describes compounds that inhibit AKR1C3 in the low nanomolar range. The compounds display 100-400 fold selectivity and act as androgen receptor antagonists in the low micromolar range. This is important because inhibitors of AKRC1 and AKRC2 are undesirable in the context of prostate cancer as inhibition of either receptor in the prostate would be predicted to promote proliferation. Compounds are available in sufficient quantity for in vitro and in vivo testing.
J Steroid Biochem Mol Biol. 2013 Sep;137:136-49.
Docket # X5724