Design, synthesis and pharmacological evaluation of 1,4-naphthoquinone- 1,2,3-triazole hybrids as new anticancer agents with multi-kinase inhibitory activity.

ABSTRACT: Targeting important oncogenic kinases that contribute to hallmarks of cancer has revolutionized cancer therapy. Ten 1,4-naphthoquinone derivatives linked to 1,2,3-triazole (4a-4j) were designed and synthesized as kinase inhibitors especially aimed at blocking CDK2, a validated and important cancer target. Assessment of the antiproliferative activity of the synthesized compounds against lung (EBC-1), pancreatic ductal adenocarcinoma (PDAC, AsPC-1 and Mia-Paca-2), colorectal (HT-29), and breast cancer (MCF-7) cells revealed that most of the derivatives possess considerable antiproliferative potential, with IC₅₀ values as low as 0.3 µM. In contrast, the compounds relatively spared NIH3T3 non-cancer cell line. The kinase inhibitory effect of the best compounds was examined against a

SUBMITTER: Mardaneh P 

PROVIDER: S-EPMC11850817 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature