Novel piperine-carboximidamide hybrids: design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway.

ABSTRACT: A new series of piperine-carboximidamide hybrids VIa-k was developed as a new cytotoxic agent targeting EGFR, BRAF, and CDK2. The antiproliferative effect against four cancer cells was investigated against erlotinib. Hybrids VIc, VIf, VIg, VIi, and VIk have the highest antiproliferative activity. Compounds VIc, VIf, VIg, VIi, and VIk inhibited EGFR with IC₅₀ values ranging from 96 to 127 nM. Compounds VIf and VIk had the most potent inhibitory activity as BRAF^V600E (IC₅₀ = 49 and 40 nM, respectively) and were discovered to be potent inhibitors of cancer cell proliferation (GI₅₀ = 44 and 35 nM against four cancer cell lines, respectively). Compound VIk, the

SUBMITTER: Al-Wahaibi LH 

PROVIDER: S-EPMC9721426 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature