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SSH Prof. Elkamhawy, in collaboration with professors from other universities has developed novel Raf kinase inhibitors for melanoma treatment

This study, published in Archives of Pharmacal Research (Top 5% JCR & SCOPUS), reports the design, synthesis, and biological evaluation of a new series of Raf kinase inhibitors targeting both B-Raf and C-Raf isoforms. Given the resistance associated with current B-Raf inhibitors, our approach focuses on dual inhibition to overcome drug resistance and enhance therapeutic efficacy.

Key Findings:

  • The synthesized compounds were evaluated for their inhibitory activity against B-RafV600E and C-Raf kinases.
  • The lead compound exhibited nanomolar IC₅₀ values against both targets and demonstrated potent antiproliferative activity in melanoma cell lines.
  • Mechanistic studies confirmed that the lead inhibitor suppressed MAPK pathway activation, leading to apoptosis in melanoma cells.
  • Selectivity profiling revealed minimal cytotoxicity in normal human fibroblasts, highlighting its potential as a safer alternative to existing therapies.

Here is the link to read the full paper.

This work contributes to the ongoing search for next-generation melanoma therapies and paves the way for further in vivo studies to validate its clinical potential.

Link to Research Group Webpage.
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