Hydroxynaphthalenecarboxamides and substituted piperazinylpropandiols, two new series of BRAF inhibitors. A theoretical and experimental study
- Campos, Ludmila Estefanía
- Garibotto, Francisco Matías
- Angelina, Emilio Luis
- Kos, Jiri
- Gonec, Tomas
- Marvanova, Pavlina
- Vettorazzi, Marcela Cristina
- Oravec, Michal
- Jendrzejewska, Izabela
- Jampilek, Josef
- Alvarez, Sergio Eduardo
- Enriz, Ricardo Daniel
DOIAbstract
The oncogenic mutated kinase BRAFV600E is an attractive molecular target because it is expressed in several human cancers, including melanoma. To present, only three BRAF small inhibitors are approved by the FDA for the treatment of patients with metastatic melanoma: Vemurafenib, Dabrafenib and Encorafenib. Although many protocol treatments have been probed in clinical trials, BRAF inhibition has a limited effectiveness because patients invariably develop resistance and secondary toxic effects associated with the therapy. These limitations highlight the importance of designing new and better inhibitors with different structures that could establish different interactions in the active site of the enzyme and therefore decrease resistance pro...
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