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Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
| Content Provider | MDPI |
|---|---|
| Author | Abdullah, Omeima |
| Copyright Year | 2021 |
| Description | Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, colon, and pancreatic cancers. Thus, inhibiting Aurora-A kinase activity is a promising approach for cancer treatment. Here, new triazole derivatives were designed as bioisosteric analogues of the known inhibitor JNJ-7706621. The new compounds showed interesting inhibitory activity against Aurora-A kinase, as attested by $IC_{50}$s in the low to submicromolar range. |
| Starting Page | 5678 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules26185678 |
| Journal | Molecules |
| Issue Number | 18 |
| Volume Number | 26 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-09-18 |
| Access Restriction | Open |
| Subject Keyword | Molecules Oncology Cancer Aurora-a Kinase Triazole |
| Content Type | Text |
| Resource Type | Article |
