Understanding the mechanism of action of pyrrolo[3,2-b]quinoxaline-derivatives as kinase inhibitors
| Title | Understanding the mechanism of action of pyrrolo[3,2-b]quinoxaline-derivatives as kinase inhibitors |
| Publication Type | Journal Article |
| Year of Publication | 2020 |
| Authors | Unzue A., Jessen-Trefzer C., Spiliotopoulos D., Gaudio E., Tarantelli C., Dong J., Zhao H., Pachmayr J., Zahler S., Bernasconi E., Sartori G., Cascione L., Bertoni F., Śledź P., Caflisch A., Nevado C. |
| Journal | RSC Medicinal Chemistry |
| Volume | 11 |
| Issue | 8 |
| Pagination | 1573-1580 |
| Date Published | 2020 Jun 30 |
| Type of Article | Research Article |
| Abstract | The X-ray structure of the catalytic domain of the EphA3 tyrosine kinase in complex with a previously reported type II inhibitor was used to design two novel quinoxaline derivatives, inspired by kinase inhibitors that have reached clinical development. These two new compounds were characterized by an array of cell-based assays and gene expression profiling experiments. A global chemical proteomics approach was used to generate the drug-protein interaction profile, which suggested suitable therapeutic indications. Both inhibitors, studied in the context of angiogenesis and in vivo in a relevant lymphoma model, showed high efficacy in the control of tumor size. |
| URL | http://dx.doi.org/10.1039/D0MD00049C |
| DOI | 10.1039/D0MD00049C |
| pubindex | 0255 |
| Short Title | RSC Med. Chem. |
| Alternate Journal | RSC Med. Chem. |
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