Mithramycin derivatives having increased selectivity and anti-cancer activity
AssigneeUniversity of Kentucky Research Foundation
InventorsJurgen Rohr, Oleg Tsodikov, Markos Leggas, Caixia Hou, Joseph Eckenrode, Prithiba Mitra, Abhisek Mandal
Life of this patent
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Abstract
Mithramycin (MTM) short side chain ketone (SK) derivatives and MTM short side chain diketone (SDK) derivatives are provided. The MTM SK and MTM SDK derivatives are useful for treatment of cancer or neuro-diseases associated with an aberrant erythroblast transformation-specific transcription factor. Unique MTM SK and MTM SDK derivatives have increased selectively toward ETS transcription factor.
Claims18
A mithramycin (MTM) short side chain ketone (SK) derivatives and MTM short side chain diketone (SDK) derivative having the following formula:
- or a pharmaceutically acceptable salt thereof, wherein R1 is ═O or —OH, and R2 is
- (a) a substituted tryptophan (Trp) or phenylalanine (Phe) derivative having a substitution on a phenyl or indole ring of the Trp or Phe derivative, wherein the substitution is selected from the group consisting of lower alkyl, prenyl, aryl, alkylaryl, alkoxyl, nitro, halogen, and halocarbon;
- (b) a substituted Trp, Phe, Trp-Phe, or Phe-Trp dipeptide derivative having a substitution on a phenyl or indole ring of the dipeptide derivative, wherein the substitution is selected from the group consisting of lower alkyl, prenyl, aryl, alkylaryl, alkoxyl, nitro, halogen, and halocarbon;
- or
- (c) an unsubstituted Trp, Phe, Trp-Phe, or Phe-Trp dipeptide derivative.
Dependencies are inferred from the claim text.