Chemistry

Prof. Elkamhawy, in collaboration with Prof. Lee’s team (Dongguk Univ., Korea) and Prof. Ammar’s group (Edinburgh Napier Univ., UK), 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.
news