Design, synthesis, and anticancer evaluation of novel pyrrole–pyrazoline/chalcone hybrids: in vitro and computational insights into EGFR inhibition

RSC Medicinal Chemistry 2026 Open access

Read full text
Authors: Mansour S. Alturki, Marwa Fawzy Elmetwaly Ahmed, Abdulaziz H. Al Khzem, Mohamed Sayed Gomaa, Mohammad Sarafroz, Nada Tawfeeq, Mashael M. Alharbi, Abdulaziz K. Al Mouslem, Mohammed F. Aldawsari, Wajin R. Alruwili, Shah Alam Khan, Radwan S. El-Haggar
+1 more Atiah H. Almalki
DOI: 10.1039/d5md00800j
Cited by: 1
References: 80

Abstract

= 0.198 μM). Flow cytometry analysis of human breast cancer cells (MCF-7) showed that 6b induces significant cell arrest in the G2/M phase. Real-time polymerase chain reaction (RT-PCR) experiments further confirmed the molecular mechanisms, revealing that 6b modulated key apoptotic regulators, significantly increasing the Bax/Bcl-2 ratio and upregulating p53, BAX, and caspase-7, while concurrently suppressing Bcl-2 expression. Molecular simulation studies provide evidence for the preferential binding of 6b to the active state of EGFR, consistent with the experimental results. The synthetic strategy used to prepare the pyrrole-pyrazoline/chalcone scaffold is simple, hence providing efficient access to the title compounds whose potential can be further explored as an EGFR-targeted anticancer chemotype.

Fields of Study & Subjects

Synthesis and biological activity Synthesis and Characterization of Pyrroles Synthesis and Biological Activity

Publication details

Journal / source
RSC Medicinal Chemistry
Publisher
Royal Society of Chemistry (RSC)
Volume
17
Issue
5
Pages
2667–2691
Publication date
1 January 2026
Language
EN