Benzimidazole derivatives as dual EGFR and BRAF^V600E inhibitors with pro-apoptotic antiproliferative potential

Lamya H. Al-Wahaibi, Mohamed Samir, Stefan Bräse, Bahaa G. M. Youssif and Martha M. Morcoss

RSC Adv., 2026,16, 25216-25228

Abstract

Compound 8d exhibited potent dual inhibitory activity against EGFR and BRAF^V600E. It induces apoptosis, with high gastrointestinal absorption.

New pyrazolylindolin-2-one based coumarin derivatives as anti-melanoma agents: design, synthesis, dual BRAF^V600E/VEGFR-2 inhibition, and computational studies

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 BRAF^V600E/VEGFR-2 inhibitors targeting melanoma cells A375. Docking simulation showed various interactions with the binding residues in BRAF^V600E and VEGFR-2 active sites.

Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAF^V600E inhibitors

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 BRAF^V600E.

Design, synthesis, in silico studies, and antiproliferative activity of a novel series of thiazole/1,2,3-triazole hybrids as apoptosis inducers and multi-kinase inhibitors endowed with anti-breast cancer activity

Fatma A. M. Mohamed, Saleha Y. M. Alakilli, Hassan H. Alhassan, Sara Osman Yousif, Eid Alatwi, Hesham A. M. Gomaa, Heba Abu Alrub, Bandar A. Alyami, Ahmed H. Abdelhafez, Stefan Bräse and Bahaa G. M. Youssif

RSC Adv., 2026,16, 3349-3367

Abstract

This study reported the development of a novel series of thiazole/1,2,3-triazole hybrids and in vitro anticancer efficacy. Compounds 10c, 10e, 10k, 10m, 10n, and 10o exhibited superior anticancer efficacy, particularly against MCF-7 breast cancer.

Design, synthesis and antiproliferative, apoptotic, and immunomodulatory properties of new heteroaryl pyridine-linked 1,2,4-oxadiazoles as prospective dual EGFR/BRAF^V600E inhibitors

Hesham A. M. Gomaa, Mohamed E. Shaker, Sami I. Alzarea, Eid Alatwi, Fatma A. M. Mohamed, Abdullah Yahya Abdullah Alzahrani, Bandar A. Alyami, Stefan Bräse, Safwat M. Rabea and Bahaa G. M. Youssif

RSC Adv., 2026,16, 14294-14309

Abstract

Vemurafenib triggers resistance via EGFR feedback upregulation, compound 21c achieves a “vertical blockade” by simultaneously inhibiting EGFR and mutant BRAF.

Benzimidazole derivatives as dual EGFR and BRAFV600E inhibitors with pro-apoptotic antiproliferative potential

Abstract

New pyrazolylindolin-2-one based coumarin derivatives as anti-melanoma agents: design, synthesis, dual BRAFV600E/VEGFR-2 inhibition, and computational studies

Abstract

Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAFV600E inhibitors

Abstract

Design, synthesis, in silico studies, and antiproliferative activity of a novel series of thiazole/1,2,3-triazole hybrids as apoptosis inducers and multi-kinase inhibitors endowed with anti-breast cancer activity

Abstract

Design, synthesis and antiproliferative, apoptotic, and immunomodulatory properties of new heteroaryl pyridine-linked 1,2,4-oxadiazoles as prospective dual EGFR/BRAFV600E inhibitors

Abstract

Benzimidazole derivatives as dual EGFR and BRAF^V600E inhibitors with pro-apoptotic antiproliferative potential

New pyrazolylindolin-2-one based coumarin derivatives as anti-melanoma agents: design, synthesis, dual BRAF^V600E/VEGFR-2 inhibition, and computational studies

Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAF^V600E inhibitors

Design, synthesis and antiproliferative, apoptotic, and immunomodulatory properties of new heteroaryl pyridine-linked 1,2,4-oxadiazoles as prospective dual EGFR/BRAF^V600E inhibitors