Palmarumycin based inhibitors of thioredoxin and methods of using same

Abstract

Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.

1 - 15 . (canceled) 
     
     
         16 . A compound, or salt thereof, having the general formula: 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is H or OH; 
         R 2  is selected from the group consisting of O(CH 2 )nCH 3 , OCH(CH 3 )CHnCH 3 , OCH 2 CH 2 -morpholino, OC(O)CH 2 NH 2 , and OC(O)CH(CH(CH 3 ) 2 )NH 2 , OC(O)CH(CH 3 )NH 2 , OC(O)CH(CH 2 Phenyl)NH 2 , OC(O)CH(CH 2  p-OHPhenyl)NH 2   
       
       
         
           
           
               
               
           
         
       
       OC(O)CH(CH 2 OH)NH 2 , OC(O)CH(CH 2 SH)NH 2 , OC(O)CH(CH 2 COOH)NH 2 , OC(O)CH(CH 2 CH 2 COOH)NH 2 , OC(O)CH(CH 2 CONH 2 )NH 2 , OC(O)CH(CH 2 CH 2 CONH 2 )NH 2 , OC(O)CH(CH(CH 3 )CH 2 CH 3 )NH 2 , OC(O)CH(CH 2 CH(CH 3 ) 2 )NH 2 , OC(O)CH(CH(OH)CH 3 )NH 2 ; and 
       
         
           
           
               
               
           
         
         n is 1-4, and 
         R 3  is hydrogen, or NHNHC(CH 3 ) 2 CONH 2 , 
            represents the option of having a double bond.