Synthesis and structure–activity relationship of N-(piperidin-4-yl)benzamide derivatives as activators of hypoxia-inducible factor 1 pathways
2018
Huang, Zhi-Ning | Liang, Han | Qiao, Hong | Wang, Bao-Rui | Zhu, Ning | Li, Hua | Zhou, Run-Run | Wang, Li-Juan | Li, Shan-Hua | Li, Fu-Nan
Guided by bioisosterism and pharmacokinetic parameters, we designed and synthesized a series of novel benzamide derivatives. Preliminary in vitro studies indicated that compounds 10b and 10j show significant inhibitory bioactivity in HepG2 cells (IC₅₀ values of 0.12 and 0.13 μM, respectively). Compounds 10b and 10j induced the expression of HIF-1α protein and downstream target gene p21, and upregulated the expression of cleaved caspase-3 to promote tumor cells apoptosis.
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