STAT3 inhibitor
Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.
1. A compound having the following structure:
wherein R 1 is selected from the group consisting of substituted or unsubstituted alkyl (C1-12) , substituted or unsubstituted heterocycloalkyl (C4-12) , acyl (C1-C6) , alkylamino (C1-6) , alkoxyamino (C1-6) ,
wherein R 1 is not —CH 3 ;
wherein X 1 is —O—or —NH—; wherein n=0, 1, 2, 3, 4, or 5; wherein R′ is selected from the group consisting of substituted or unsubstituted alkyl (C1-6) , alkylamino (C1-6) , halogen, —OH, amido (C1-12) , alkylsulfonylamino (C1-12) ,
substituted or unsubstituted heterocycloalkyl (C4-12) ; wherein R 11 and R 12 are each independently —H or alkyl (C1-6) ; wherein R″ is —H, —OH, —NH 2 , or halogen; wherein R′″ is alkyl (C1-6) ;
wherein R 2 is selected from the group consisting of —NO 2 , —NH 2 , H, amido (C1-12) , substituted amido (C1-12) , alkylsulfonylamino (C1-12) , dialkylsulfonylamino (C1-12) , and halogen; wherein R 3 and R 4 are halogen;
or a salt thereof.
2. The compound of claim 1 , wherein R 2 , is —NO 2 .
3. The compound of claim 1 , wherein R 3 , and R 4 are —Cl.
4. The compound of claim 1 , wherein R 1 , is selected from the group consisting of:
—OAc, and —OH.
5. The compound of claim 4 , wherein R 1 is selected from the group consisting of:
6. The compound of claim 1 , wherein R 2 is selected from the group consisting of:
—NH 2 ,
—H, —NHAc, —N(Ms) 2 , and —NHMs.
7. The compound of claim 1 , wherein the compound has a structure selected from the group consisting of:
8. The compound claim 7 , wherein the compound has a structure selected from the group consisting of:
9. The compound of claim 1 , wherein R 1 is
and wherein R′ is —NMe 2 , —NHMe, —NHAc,
10. The compound of claim 1 , wherein the compound has the structure
wherein n=1, 2, 3, or 4; wherein R′ is —NMe 2 , —NHMe, —NHAc,
11. The compound of claim 1 , wherein the compound has the structure:
wherein R′ is —NMe 2 , —NHMe, —NHAc,
12. The compound of claim 1 , wherein the compound has the structure
wherein R′ is —NMe 2 , —NHMe, —NHAc,
and
wherein R″ is —H, —NH 2 , or —Cl.
13. The compound of claim 1 , wherein the compound has the structure:
wherein R′ is —NMe 2 , —NHMe, —NHAc,
and
wherein R′″ is -Et or -i-Pr.
14. The compound of claim 1 , wherein R 1 is selected form the group consisting of
15. The compound of claim 14 , wherein the compound has the structure
16. The compound of claim 1 , wherein the compound has the structure