New benzimidazole-triazole glycoconjugates as anti-cancer agents and EGFR inhibitors.

ABSTRACT: A new series of glycosyl heterocyclic scaffolds, 5a-10b with N-glycosidic linkage, were synthesized, starting with 2-acetyl-1H-benzimidazole as a precursor of the propargyl-derived substrates (2) and (3), which were then converted to the target 1,2,3-triazole glycosides (8a-10b) bearing unprotected hydroxyl groups. The new chemical entities have been assessed for their cytotoxic properties on diverse human cancer cell lines, namely HepG-2 (human liver cancer), HCT-116 (human colorectal), and MCF-7 (human breast cancer), in addition to a human normal cell line (BJ-1), following the LDH assay and with erlotinib and doxorubicin as the standard references. Most of the tested compounds demonstrated potent activity, particularly the triazole glycosides 6b, 7b, 8b, 9a, 9b, 10a, and 10b. Compound

SUBMITTER: Srour AM 

PROVIDER: S-EPMC12264064 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature