Granted Patent
B2
US 12,415,822 · App. 18/106,543 · Granted Sep 16, 2025
Small molecule inhibitors selective for polo-like kinase protein
Assignee:
University of South Carolina
C07F9/222A61P35/00C07C233/66C07C233/80C07C233/81C07C235/84C07C311/46C07F5/04A61K31/167A61K31/196A61P35/04
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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 (18)
1. A method for inhibiting Polo-like Kinase proteins, the method comprising:
providing a small molecule PLK inhibitor to a medium containing one or more Polo-like Kinase proteins, wherein the small molecule PLK inhibitor has the following structure:
wherein
R 1 comprises an alkyl, —O-alkyl, —S-alkyl, or —NH-alkyl, and optionally includes a terminal aryl;
R 7 is selected from:
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 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.
5. The method of claim 1 , wherein the one or more Polo-like Kinase proteins comprise PLK1.
6. The method of claim 1 , wherein the one or more Polo-like Kinase proteins comprise PLK3.
7. 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.
8. The method of claim 1 , wherein R 1 comprises a C10 to C12 alkyl.
9. The method of claim 1 , wherein the small molecule PLK inhibitor has an atomic mass of about 1000 Daltons or less.
10. The method of claim 1 , wherein the small molecule PLK inhibitor has an atomic mass of about 500 Daltons or less.
11. The method of claim 1 , wherein the small molecule PLK inhibitor has a polar surface area of about 200 Å or less.
12. The method of claim 1 , wherein the small molecule PLK inhibitor has a polar surface area of about 100 Å or less.
13. A method for inhibiting Polo-like Kinase proteins, the method comprising:
providing a small molecule PLK inhibitor to a medium containing one or more Polo-like Kinase proteins, wherein the small molecule PLK inhibitor has the structure of one or more of:
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Feb 7, 2023
From: MCINNES, CAMPBELL; CRAIG, SANDRA NAVONNE
To: UNIVERISTY OF SOUTH CAROLINA
Reel/Frame 062610/0461 →
Continuity (4)
Provisional Application
62318439
· Apr 5, 2016
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