IP Library Granted Patent US 10,457,639
Granted Patent B2
US 10,457,639 · App. 13/059,183 · Granted Oct 29, 2019

Fluorescent regulators of RASSF1A expression and human cancer cell proliferation

Inventors: Milton L. Brown (Brookeville, MD); Kathryn D. Sheikh (Washington, DC); Mikell A. Paige (Fairfax, VA); Partha Banerjee (Rockville, MD); Shankar Jagadeesh (Gaithersburg, MD)
Assignee: GEORGETOWN UNIVERSITY
C07D209/88A61K31/403A61K45/06
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Quick Facts
Patent No.
US 10,457,639
App. No.
13/059,183
Granted
Oct 29, 2019
Kind
B2
Abstract

The invention provides methods for the treatment of cancer in a subject comprising administering a dansyl-carbazole compound.

Claims (20)

1. A compound that has the structure:

2. A method for treating a cancer in a subject, the method comprising: administering to a subject in need of such treatment a therapeutically effective amount of a composition comprising the compound of claim 1 to treat the cancer in the subject.

3. The method of claim 2 , wherein treatment suppresses further growth of the cancer.

4. The method of claim 2 , wherein treatment results in regression of the cancer.

5. The method of claim 2 , wherein the cancer comprises cancer cells with decreased Ras-association domain family IA (RASSF1A) expression.

6. The method of claim 5 , wherein the Ras-association domain family IA (RASSF1A) expression is decreased by an increase in methylation of the promoter for RASSF1A.

7. The method of claim 5 , wherein administration of the composition increases Ras-association domain family IA (RASSF1A) expression.

8. A method for suppressing the growth of a cell, the method comprising: contacting the cell with a composition comprising the compound of claim 1 to suppress the growth of the cell.

9. A method for reducing DNA methyltransferase activity in a cell, the method comprising: contacting the cell with a composition comprising the compound of claim 1 to reduce DNA methyltransferase activity in the cell.

10. The method of claim 9 , wherein the DNA methyltransferase activity is reduced by reducing the activity of DNA methyltransferase 3b (DNMT-3b).

11. A method for increasing Ras-association domain family IA (RASSF1A) expression in a cell, the method comprising: contacting the cell with a composition comprising the compound of claim 1 to increase RASSF1A expression in the cell.

12. The method of claim 11 , wherein the cell has decreased Ras-association domain family IA (RASSF1A) expression.

13. The method of claim 8 , wherein the cell is a cancer cell.

14. A method of identifying a cell in which Ras-association domain family IA (RASSF1A) expression is decreased, the method comprising: contacting the cell with a composition comprising the compound of claim 1 , wherein if the compound is retained in the cell, the cell is identified as having decreased RASSF1A expression.

15. A method of determining if one or more cells from a subject are cancer cells, the method comprising: obtaining one or more cells from a subject, contacting the one or more cells with a composition comprising the compound of claim 1 , measuring the fluorescence of the one or more cells, wherein if the fluorescence of the one or more cells is indicative of the presence of the compound, the one or more cells is identified as being a cancer cell.

16. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

17. The pharmaceutical composition of claim 16 , further comprising one or more additional anti-cancer compounds.

18. A kit comprising a pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , and instructions for preparation and/or administration of the pharmaceutical composition.

19. The kit of claim 18 , further comprising one or more additional anti-cancer compounds.

20. A prodrug of the compound of claim 1 , wherein the prodrug comprises the compound and (a) a group attached to the compound as a carboxylate ester, wherein the group is alkyl, aryl, aralkyl, acyloxyalkyl, alkoxycarbonyloxyalkyl, or (b) a group attached to the compound as an ester of hydroxyl, thiol, or amine, wherein the group is an acyl group, an alkoxycarbonyl, aminocarbonyl, phosphate, or sulfate.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 20, 2011
From: BROWN, MILTON L.; SHEIKH, KATHRYN D.; PAIGE, MIKELL A.; BANERJEE, PARTHA; JAGADEESH, SHANKAR
To: GEORGETOWN UNIVERSITY
Reel/Frame 026624/0122 →
Continuity (2)
Provisional Application 61189059 · Aug 15, 2008
Related Publication 20110152339A1 · Jun 23, 2011