Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors
View Patent ↗Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
1. A compound having the formula (I):
or a salt thereof, wherein:
n is an integer from 1 to 12;
m and p are independently an integer from 1 to 5;
q is 0 or 1;
each R 1 is independently selected from the group consisting of;
C 1 -C 8 substituted or unsubstituted alkyl, C 4 -C 15 substituted or unsubstituted cycloalkyl, C 3 -C 15 substituted or unsubstituted branched alkyl, C 6 -C 20 substituted or unsubstituted aryl, C 6 -C 20 substituted or unsubstituted heteroaryl, C 7 -C 24 substituted or unsubstituted aralkyl, and C 7 -C 24 substituted or unsubstituted heteroaralkyl and,
each R 2 is independently selected from hydrogen or a C 1 -C 8 substituted or unsubstituted alkyl.
2. The compound of claim 1 , wherein the compound is a compound listed in Table A.
3. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
4. A kit comprising the compound of claim 1 and instructions for use as an anticancer or antiparasitic agent.
5. A method of inhibiting a histone demethylase, comprising administering an amount of a compound of claim 1 , wherein the amount of the compound is sufficient to inhibit the histone demethylase by at least about 50%.
6. A method of treating a parasitic infection, comprising administering a compound of claim 1 in a therapeutically effective amount.
7. The method of claim 5 , wherein the enzyme is lysine-specific demethylase-1.
8. A compound of claim 1 , wherein the compound is
9. A pharmaceutical composition of claim 3 wherein the compound is
10. A kit of claim 4 wherein the compound is
11. A method of claim 5 wherein the compound is:
12. A method of claim 6 wherein the compound is: