Version 1
: Received: 25 April 2024 / Approved: 26 April 2024 / Online: 26 April 2024 (16:58:58 CEST)
How to cite:
Guerra, F.S.; Freitas, R.H.C.N.D.; Moldovan, F.; Rocha, D.R.; Fernandes, P.D. Design, Synthesis and In Vitro Analysis of New Vemurafenib Analogs. Preprints2024, 2024041757. https://doi.org/10.20944/preprints202404.1757.v1
Guerra, F.S.; Freitas, R.H.C.N.D.; Moldovan, F.; Rocha, D.R.; Fernandes, P.D. Design, Synthesis and In Vitro Analysis of New Vemurafenib Analogs. Preprints 2024, 2024041757. https://doi.org/10.20944/preprints202404.1757.v1
Guerra, F.S.; Freitas, R.H.C.N.D.; Moldovan, F.; Rocha, D.R.; Fernandes, P.D. Design, Synthesis and In Vitro Analysis of New Vemurafenib Analogs. Preprints2024, 2024041757. https://doi.org/10.20944/preprints202404.1757.v1
APA Style
Guerra, F.S., Freitas, R.H.C.N.D., Moldovan, F., Rocha, D.R., & Fernandes, P.D. (2024). Design, Synthesis and In Vitro Analysis of New Vemurafenib Analogs. Preprints. https://doi.org/10.20944/preprints202404.1757.v1
Chicago/Turabian Style
Guerra, F.S., David Rodrigues Rocha and Patricia Dias Fernandes. 2024 "Design, Synthesis and In Vitro Analysis of New Vemurafenib Analogs" Preprints. https://doi.org/10.20944/preprints202404.1757.v1
Abstract
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.
Biology and Life Sciences, Biochemistry and Molecular Biology
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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