High-throughput computational screening and <i>in vitro</i> evaluation identifies 5-(4-oxo-4H-3,1-benzoxazin-2-yl)-2-[3-(4-oxo-4H-3,1-benzoxazin-2-yl) phenyl]-1H-isoindole-1,3(2H)-dione (C3), as a novel EGFR

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High-throughput computational screening and <i>in vitro</i> evaluation identifies 5-(4-oxo-4H-3,1-benzoxazin-2-yl)-2-[3-(4-oxo-4H-3,1-benzoxazin-2-yl) phenyl]-1H-isoindole-1,3(2H)-dione (C3), as a novel EGFR—HER2 dual inhibitor in gastric tumors

2023; Cognizant Communication Corporation; Volume: 32; Issue: 2 Linguagem: Inglês

10.32604/or.2023.043139

ISSN

1555-3906

Autores

Mesfer Al Shahrani, Reem M. Gahtani, Mohammad Abohassan, Mohammad Y. Alshahrani, Yasser Alraey, Ayed A. Dera, Mohammed Asiri, Prasanna Rajagopalan,

Tópico(s)

Synthesis and pharmacology of benzodiazepine derivatives

Resumo

Gastric cancers are caused primarily due to the activation and amplification of the EGFR or HER2 kinases resulting in cell proliferation, adhesion, angiogenesis, and metastasis. Conventional therapies are ineffective due to the intra-tumoral heterogeneity and concomitant genetic mutations. Hence, dual inhibition strategies are recommended to increase potency and reduce cytotoxicity. In this study, we have conducted computational high-throughput screening of the ChemBridge library followed by

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High-throughput computational screening and <i>in vitro</i> evaluation identifies 5-(4-oxo-4H-3,1-benzoxazin-2-yl)-2-[3-(4-oxo-4H-3,1-benzoxazin-2-yl) phenyl]-1H-isoindole-1,3(2H)-dione (C3), as a novel EGFR—HER2 dual inhibitor in gastric tumors