In vitro study shows that five vemurafenib analogs induce death and inhibit migration in A375 melanoma cells, suggesting prolonged activity against BRAF V600E metastatic melanoma.
Metastatic melanoma patients have a poor prognosis with poor responsiveness to chemotherapy. BRAF V600E mutations have been detected in ~40% of melanoma patients. Vemurafenib is an oral agent licensed for patients with BRAF V600E mutation-positive inoperable and metastatic melanoma, which already presents resistance that leads to patient relapse and the serious side effects. In our study, we synthesized 5 new vemurafenib analogs, RF-86A, RF-87A, RF-94A, RF-94B and RF-96B, with structural improve-ments, in order to increase the anti-proliferative and anti-metastatic effect on human melanoma. We showed that the analogs were efficient in inducing cell death and reducing the migration of A375 cells, by inhibition of MMP-2 and MMP-9 activity, indicating that this action may be longer lasting comparing to the action of Vemurafenib.
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Guerra et al. (2024) studied this question.
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