EZR–ROS1 rearrangement as a novel mechanism of acquired resistance to EGFR-TKIs in NSCLC: a case report and literature review

ROS1 rearrangement is a rare mechanism of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), with an incidence o 1 Introduction Non-small cell lung cancer (NSCLC) remains the leading cause of cancer-related deaths worldwide (1). Among its...

Targeting EGFR With Quinazoline‐4‐One/Chalcone Hybrids: Design, Synthesis, and Anticancer Evaluation

A series of novel quinazoline-4-one/chalcone hybrids were synthesized and evaluated as epidermal growth factor receptor (EGFR) inhibitors with promising anticancer activity. Archiv der PharmazieVolume 359, Issue 1 e70186 FULL PAPER Targeting EGFR With Quinazoline-4-One/Chalcone Hybrids: Design, Synthesis, and Anticancer Evaluation...

Targeting EGFR With Quinazoline‐4‐One/Chalcone Hybrids: Design, Synthesis, and Anticancer Evaluation

A series of novel quinazoline-4-one/chalcone hybrids were synthesized and evaluated as epidermal growth factor receptor (EGFR) inhibitors with promising anticancer activity. Archiv der PharmazieVolume 359, Issue 1 e70186 FULL PAPER Targeting EGFR With Quinazoline-4-One/Chalcone Hybrids: Design, Synthesis, and Anticancer Evaluation...

In silico evaluation of (benzo)chromeno[3,4-c]pyridine derivative as dual EGFR/HER2 inhibitors for non-small cell lung cancer

(Benzo)chromeno[3,4-c]pyridine derivatives continue to attract significant scientific interest due to their broad pharmacological relevance, especially in cancer chemotherapy. In this study, both experimental and density functional theory (DFT) based computational approaches were employed to investigate the structural, electronic, spectroscopic, and...

Hoth Therapeutics Delivers 100% Clinical Response with ~50% Reduction in Disease Severity in Open-Label PK Cohort of EGFR-Treated Cancer Patients

Primary endpoint ARIGA improved by ~50% from baseline by Week 6, with all evaluable patients reaching low-severity disease; additional endpoints demonstrated ~34% improvement in oncology toxicity (CTCAE) and ~37% reduction in patient-reported pruritus. NEW YORK, Jan. 22, 2026 /PRNewswire/ --...

A genome-wide genetic screen reveals the P2Y2-integrin axis as a stabilizer of EGFR mutants in non–small cell lung cancer (NSCLC)

AbstractActivating mutations in the epidermal growth factor receptor (EGFR) gene drive non–small cell lung cancer (NSCLC). Oncogenic EGFR mutants are ligand-independent and more stable, but the underlying mechanism remains unclear. We hypothesized that EGFR mutants selectively leverage cellular stabilizers to...

Novel pyrazole–oxadiazole–chalcone/oxime hybrids as dual EGFR/VEGFR-2 inhibitors with promising anticancer potential: a comprehensive cytotoxicity evaluation, mechanistic insights and SAR analysis

Abstract A novel series of pyrazole–1,3,4-oxadiazole hybrids incorporating chalcone/oxime scaffolds (10a–10c, 11a–11c, 12a–12i, 13a–13i, and 14a–14i) was synthesized and subjected to an detailed cytotoxicity profile against the NCI-60 human cancer cell line panel. Several derivatives demonstrated broad-spectrum growth inhibition, with...

Design and synthesis of novel thiazole/1,2,4-triazole/quinoline hybrids as antiproliferative agents, apoptosis inducers, immunomodulators, and multi-EGFR/BRAFV600E/HER-2 inhibitors

Abstract We developed a novel category of quinoline-based compounds that operate as multi-target inhibitors of EGFR, HER-2, and BRAFV600E. The new compounds’ antiproliferative activity was tested against four cancer cell lines. All compounds had GI50 values ranging from 25 to...