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Article

Discovery of novel diaryl urea-oxindole hybrids as BRAF kinase inhibitors targeting BRAF and KRAS mutant cancers.

Bioorganic chemistry - 1 Dec 2024

Ghannam Iman A Y, El Kerdawy Ahmed M, Mounier Marwa M, Abo-Elfadl Mahmoud T, Abdel-Mohsen Heba T

Abstract excerpt

In the current study, a novel series of diaryl urea incorporating oxindole moiety was rationally designed as type II BRAF inhibitors targeting BRAF and KRAS mutant cancers. Molecular hybridization between the diaryl urea scaffold which binds to the inactive conformation of protein kinases on one side and the oxindole core which exhibit adenine mimic properties to be settled in the hinge region on the other side...

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Identifiers

PMID: 39368145
DOI: 10.1016/j.bioorg.2024.107848

Genes

BRAF
KRAS

Variants

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