Discovery of novel dehydroabietylamine-pyrimidine hybrids: design, synthesis and anti-tumor evaluation.

ABSTRACT: Challenges in cancer treatment lie in the identification and development of novel agents with potent anti-tumor activity. A series of novel dehydroabietylamine-pyrimidine derivatives 3a-3s were designed and synthesized based on the principles of molecular hybridization. The inhibitory activities of the target compounds against the proliferation of four different human cancer cell lines (HepG2, A549, HCT116 and MCF-7) were evaluated. Among them, compound 3r, which contains a bicyclic quinuclidine ring, was identified as a potent apoptotic inducer, with a better IC₅₀ value of 1.15 ± 0.31 μM on MCF-7 cells and a favorable selectivity index (SI = 27.7) on human normal mammary epithelial cells (MCF-10A). Cell clonogenic and migration assays further demonstrated that 3r not only effec

SUBMITTER: Zhang ZW 

PROVIDER: S-EPMC12409675 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature