Coumarin-modified androgens for the treatment of prostate cancer
AssigneesHealth Research, Inc., University of Kentucky Research Foundation
InventorsJames L. MOHLER, Michael V. FIANDALO, David WATT, Vitaliy SVIRIPA
Life of this patent
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Abstract
Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and/or hyperplastic cells and/or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and/or hyperplastic cell growth and/or molecular imaging of malignant cells and/or hyperplastic cells and/or inducing degradation of a target protein. Also provided are compositions.
Claims56
A compound having the following structure:
- wherein
- R1 is hydrogen or an alkyl group;
- R3 is chosen from a carbonyl,
- wherein X is hydroxyl and Y is hydrogen or an alkyl group or X and Y together are a spiro-fused, substituted or unsubstituted coumarin group or coumarin isostere group, and L3 is optional and is a linking group;
- R4 is chosen from a carbonyl,
- wherein L1 is a linking group, L2 is optional and is a linking group, Z is an end group comprising a substituted or unsubstituted carbocyclic group or a substituted or unsubstituted heterocyclic group or substituted or unsubstituted coumarin group or substituted or unsubstituted coumarin isostere group, and R2 is an alkyl group or hydrogen;
- and
- R5 is a photoactive group,
- with the proviso that when R3 is a carbonyl or
- wherein X is hydroxyl and Y is hydrogen or an alkyl group, that R4 is not
- or a carbonyl.
Dependencies are inferred from the claim text.