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New quinazoline-[1,2,4]triazolo[3,4-<i>b</i>][1,3,4]thiadiazines as inhibitors of EGFR: synthesis, anti-breast cancer evaluation and <i>in silico</i> studies.


ABSTRACT: Breast cancer is the most frequently diagnosed malignancy in women. Invasive breast cancer will be diagnosed in approximately one in every eight women during their lifetime. Quinazoline-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were designed and synthesized using a pharmacophore hybridization technique that combined biologically active scaffolds. In vitro assays of the synthesized compounds' cancer activity against three breast cancer cell lines: MCF-7, MDA-MB-231, and MDA-MB-468, compounds 6i, 6k, and 6l exhibited significant activity. Compounds 6j and 6m exhibited equivalent efficacy relative to the standard drug against the MDA-MB-231 cell line, but compound 6i showed significant activity against the MDA-MB-468 cell line. Moreover, compound 6i (IC50 = 0.37 ± 0.0

SUBMITTER: Bandgar MD 

PROVIDER: S-EPMC12272992 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature