Myc g-quadruplex stabilizing small molecules and their use

Abstract

Methods for treating a tumor, such as a benign or malignant tumor, are disclosed herein. The methods include administering a therapeutically effective amount of a small molecule that selectively binds to and stabilizes G-quadruplex DNA in the promoter of the c-MYC gene to the subject. The methods are also of use to decrease the size and/or number of metastases. Compounds for use in the disclosed methods are also provided.

We claim: 
     
         1 . A method of treating cancer in a subject, comprising administering to the subject a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, having a structure of: 
       
         
           
           
               
               
           
         
         and wherein the cancer is cancer with overexpression of the c-Myc gene. 
       
     
     
         2 . The method of  claim 1 , wherein administering the therapeutically effective amount of the compound or the pharmaceutically acceptable salt thereof to the subject decreases growth and/or proliferation of the cancer. 
     
     
         3 . The method of  claim 1 , wherein the cancer is selected from leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer, and multiple myeloma. 
     
     
         4 . A method of decreasing c-Myc expression in a cell, comprising contacting the cell with an effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 
       
         
           
           
               
               
           
         
       
     
     
         5 . The method of  claim 4 , wherein the cell is in vitro. 
     
     
         6 . The method of  claim 4 , wherein the cell is in vivo. 
     
     
         7 . The method of  claim 4 , wherein decreasing expression of c-Myc in the cell decreases growth and/or proliferation of the cell. 
     
     
         8 . The method of  claim 4 , wherein the cell is a cell with overexpression of the c-MYC gene.