IP Library Granted Patent US 11,597,737
Granted Patent B2
US 11,597,737 · App. 17/001,167 · Granted Mar 7, 2023

Small molecule inhibitors selective for polo-like kinase proteins

Inventors: Campbell McInnes (Irmo, SC); Sandra Navonne Craig (Ellerbe, NC)
Assignee: University of South Carolina
C07F9/222A61P35/00C07C233/66C07C233/80C07C233/81C07C235/84C07C311/46C07F5/04A61K31/167A61K31/196A61P35/04
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Quick Facts
Patent No.
US 11,597,737
App. No.
17/001,167
Filed
Aug 24, 2020
Granted
Mar 7, 2023
Kind
B2
Art Unit
1626
USPC
514/7.5
Abstract

Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.

Claims (16)

1. A method for inhibiting Polo-Like Kinase (PLK) proteins, the method comprising:

providing a small molecule PLK inhibitor to a medium containing one or more PLK proteins, wherein the small molecule PLK inhibitor has the general structure:

wherein

R1 is an -S-alkyl; and

R 4 is an alkyl.

2. The method of claim 1 , wherein the medium comprises a solution.

3. The method of claim 1 , wherein the medium comprises one or more cells.

4. The method of claim 3 , wherein the one or more cells comprise HeLa cervical cancer cells, PTEN-deficient prostate cancer PC3 cells, KRAS mutant lung cancer A-549 cells, or a combination thereof.

5. The method of claim 1 , wherein the medium comprises one or more cells and the inhibitor induces apoptosis in a least a portion of the one or more cells.

6. The method of claim 1 , wherein the one or more Polo-like Kinase proteins comprise PLK3.

7. The method of claim 1 , wherein the one or more Polo-like Kinase proteins comprise PLK1.

8. The method of claim 1 , wherein the small molecule PLK inhibitor has an atomic mass of about 1000 Daltons or less.

9. The method of claim 1 , wherein the small molecule PLK inhibitor has an atomic mass of about 500 Daltons or less.

10. The method of claim 1 , wherein the small molecule PLK inhibitor has a polar surface area of about 200 Å or less.

11. The method of claim 1 , wherein the small molecule PLK inhibitor has a polar surface area of about 100 Å or less.

12. The method of claim 1 , wherein R4 is a methyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 24, 2020
From: MCINNES, CAMPBELL; CRAIG, SANDRA NAVONNE
To: UNIVERSITY OF SOUTH CAROLINA
Reel/Frame 053578/0315 →
Continuity (3)
Continuation 15479373 · Apr 5, 2017
Provisional Application 62318439 · Apr 5, 2016
Related Publication 20200399297A1 · Dec 24, 2020