Compounds and methods for degrading rcor1, lsd1, hdac1 and hdac2 in the corest
AssigneeUniversity of Florida Research Foundation, Inc.
InventorDaiqing LIAO
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Abstract
Described herein are compounds methods for reducing the amount of rest compressor 1 (RCOR1, also known as CoREST1), lysine-specific histone demethylase 1A (LSD1, also known as KDM1A), histone deacetylase 1 (HDAC1), histone deacetylase 2 (HDAC2) or any combination thereof in a subject. These proteins are core subunits of the CoREST complex that has both lysine deacetylase and lysine demethylase activity. By reducing the amount of RCOR1, LSD1, HDAC1 and/or HDAC2, cancer cell proliferation and tumor growth are impaired. In one aspect, the compounds useful herein have the formula I or the pharmaceutically acceptable salt thereof.
Claims24
A method for reducing the amount of rest compressor 1 (RCOR1), lysine-specific histone demethylase 1A (LSD1), histone deacetylase 1 (HDAC1), histone deacetylase 2 (HDAC2), or any combination thereof in a subject comprising administering to the subject a compound of formula I or the pharmaceutically acceptable salt thereof
- wherein X and Y are independently N or CR2,
- wherein R1 and R2 are independently hydrogen, an alkyl group, a halo group, an ester group,
- R5 is a C1 to C10 alkyl group;
- and
- n is an integer from 0 to 3.
(canceled)
A method for treating cancer in a subject comprising administering to the subject in need thereof a compound of formula I or the pharmaceutically acceptable salt thereof
- wherein X and Y are independently N or CR2,
- wherein R1 and R2 are independently hydrogen, an alkyl group, a halo group, or a carbonyl group,
- R5 is a C1 to C10 alkyl group;
- and
- n is an integer from 0 to 3.
Dependencies are inferred from the claim text.