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US 2018/0002371 A1Published application
Bufalin phosphate prodrugs and methods of use thereof
AssigneeBaylor College of Medicine
InventorsJin WANG, Jianming XU, David Michael LONARD, Bert W. O'MALLEY, Timothy Gerald PALZKILL
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Abstract
Bufalin phosphate prodrugs are provided herein, as well as methods for their use as small molecule inhibitors of steroid receptor coactivator (SRC) family proteins. Methods for using bufalin phosphate prodrugs in treating or preventing cancer are also provided herein.
Claims36
A compound of the following formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- X1 and X2 are each independently selected from the group consisting of hydrogen and
- wherein R1 and R2 are each independently selected from the group consisting of hydroxy, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted heteroalkyloxy, substituted or unsubstituted heteroalkenyloxy, substituted or unsubstituted heteroalkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted cycloalkyloxy, substituted or unsubstituted heterocycloalkyloxy, and substituted or unsubstituted amino;
- and
- wherein X1 and X2 are not simultaneously hydrogen.
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A method of identifying a subject at risk for developing a poor prognosis cancer, comprising:
- (a) obtaining a biological sample from a subject;
- and
- (b) detecting the expression of SRC-3 in the subject, wherein an increase in expression of SRC-3 in the subject as compared to SRC-3 in a control subject is indicative of a subject at risk for developing a poor prognosis cancer.
Dependencies are inferred from the claim text.