Substituted tetrahydroisoquinoline ethylbenzamide anti-cancer agents
AssigneeFlorida A&M University
InventorsKinfe Ken Redda, Suresh Kumar V. K. Eyunni
Life of this patent
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Abstract
The compounds herein disclosed are N-substituted tetrahydroisoquinoline ethylbenzamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline ethylbenzamide compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6- to 10-fold less than the IC50 of Tamoxifen.
Claims23
A substituted tetrahydroisoquinoline ethylbenzamide having the formula I:
- wherein:
- R1 and R2 are each independently a hydrogen, a halogen, a methoxy, hydroxyl, cyano, an acyl, a sulfamate, an ethylbenzamide group, an ethylbenzoate group, or an acetamido group;
- R3 is hydrogen or a furyl group, wherein when R3 is a furyl group, R1 and R2 are each a hydrogen.
The pharmaceutically acceptable composition of claim 5, wherein the compound is selected from the group consisting of:
A pharmaceutically acceptable composition comprising a substituted tetrahydroisoquinoline ethylbenzamide having the formula I:
- wherein:
- R1 and R2 are each independently a hydrogen, a halogen, a methoxy, hydroxyl, cyano, an acyl, a sulfamate, an ethylbenzamide group, an ethylbenzoate group, or an acetamido group;
- R3 is hydrogen or a furyl group, wherein when R3 is a furyl group, R1 and R2 are each a hydrogen;
- and
- a pharmaceutically acceptable carrier.
A method of inhibiting the proliferation of a cell comprising contacting a cell with an effective amount of a substituted tetrahydroisoquinoline ethylbenzamide having the formula I:
- wherein:
- when R2 and R3 are each hydrogen, R1 can be a halogen;
- when R1 and R3 are each hydrogen, R2 can be selected from the group consisting of a halogen, a cyano, or a sulfamate;
- and
- when R1 and R2 are each a hydrogen, R3 can be a furyl group;
- and
- a pharmaceutically acceptable carrier, thereby reducing the proliferation rate of the cell compared to the proliferation rate of a cell not in contact with the compound.
Dependencies are inferred from the claim text.