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.

ABSTRACT: A new series of 5-substituted-3-ethylindole-2-carboxamides 5a-k and 6a-c was designed and synthesised in an attempt to develop a dual targeted antiproliferative agent. Various spectroscopic methods of analysis were used to confirm the structures of the new compounds. The antiproliferative effect of compounds 5a-k and 6a-c against four cancer cell lines was investigated. Compounds 5a-k and 6a-c had significant antiproliferative activity against the four cancer cell lines tested, with mean GI₅₀ values ranging from 37 nM to 193 nM. The most powerful derivatives were compounds 5g, 5i, and 5j, with GI₅₀ values of 55 nM, 49 nM, and 37 nM, respectively, in comparison to the reference erlotinib, which had a GI₅₀ of 33 nM. The four most potent compounds, 5c, 5g, 5i,

SUBMITTER: Mohamed FAM 

PROVIDER: S-EPMC10131667 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature