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Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action

Fatma A. Mohamed, Saleha Y. M. Alakilli, Eman Fawzy El Azab, Faris Baawad, Esraa Ibrahim A. Shaaban, Heba Abu Alrub, Omnia M. Hendawy, Hesham A. M. Gomaa, Adel G. Bakr, Mostafa Abdelrahman, Laurent Trembleau, Anber F. Mohammed, Bahaa G. M. Youssif

2023RSC Medicinal Chemistry14 citationsDOIOpen Access PDF

Abstract

values of 46 ± 05 nM and 33 ± 04 nM, respectively. The EGFR and CDK2 assays revealed that compounds 5i and 5j displayed potent antiproliferative activity and can be considered as potential dual EGFR and CDK2 inhibitors.

Topics & Concepts

Indole testEpidermal growth factor receptorCyclin-dependent kinase 2ChemistryKinaseDual (grammatical number)EGFR inhibitorsCancer researchStereochemistryCombinatorial chemistryPharmacologyBiochemistryBiologyReceptorProtein kinase AArtLiteratureHER2/EGFR in Cancer ResearchBioactive Compounds and Antitumor AgentsCancer therapeutics and mechanisms
Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action | Litcius