Ahmed Sabt, Mohammed A. Khedr, Wagdy M. Eldehna, Abdelsamed I. Elshamy, Mohamed F. Abdelhameed, Rasha M. Allam and Rasha Z. Batran
RSC Adv., 2024,14, 5907-5925
Abstract
New pyrazolylindolin-2-one linked coumarin derivatives were designed as dual BRAFV600E/VEGFR-2 inhibitors targeting melanoma cells A375. Docking simulation showed various interactions with the binding residues in BRAFV600E and VEGFR-2 active sites.
Lamya H. Al-Wahaibi, Bahaa G. M. Youssif, Hesham A. Abou-Zied, Stefan Bräse, Alan B. Brown, Hendawy N. Tawfeek and Essmat M. El-Sheref
RSC Med. Chem., 2024,15, 2538-2552
Abstract
A series of new pyrazolylquinolin-2-ones were designed and synthesised. The structures of the new compounds were validated by IR, NMR, and elemental analysis. The new compounds were evaluated as antiproliferative agents targeting EGFR and BRAFV600E.
Ankit Kumar Singh, Jurica Novak, Adarsh Kumar, Harshwardhan Singh, Suresh Thareja, Prateek Pathak, Maria Grishina, Amita Verma, Jagat Pal Yadav, Habibullah Khalilullah, Vikas Pathania, Hemraj Nandanwar, Mariusz Jaremko, Abdul-Hamid Emwas and Pradeep Kumar
RSC Adv., 2022,12, 30181-30200
Abstract
Design of pyrimidine–sulfonamide hybrids as selective BRAFV600E inhibitors using 3D-QSAR, molecular docking and MD simulations.
Lamya H. Al-Wahaibi, Aliaa M. Mohassab, Safwat M. Rabea, Bahaa G. M. Youssif, Stefan Bräse and Essmat M. El-Sheref
RSC Adv., 2025,15, 38229-38242
Abstract
A novel series of quinolines 5a–l was investigated for antiproliferative efficacy as multi-EGFR/HER-2/BRAFV600E inhibitors. This work addresses the synthesis of a new series of pyrano[3,2-c]quinoline-3-carbonitriles 5a–l.
Daniel S. J. Miller, Sabine A. Voell, Izidor Sosič, Matic Proj, Olivia W. Rossanese, Gregor Schnakenburg, Michael Gütschow, Ian Collins and Christian Steinebach
RSC Med. Chem., 2022,13, 731-736
Abstract
Novel BRAFV600E PROTACs were developed that maintain target degradation while sparing paradoxical activation of the MAPK pathway in BRAFwt cells.