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KMID : 0043320180410121149
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Archives of Pharmacal Research
2018 Volume.41 No. 12 p.1149 ~ p.1161
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Synthesis and structure?activity relationship of N-(piperidin-4-yl)benzamide derivatives as activators of hypoxia-inducible factor 1 pathways
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Huang Zhi-Ning
Liang Han
Qiao Hong
Wang Bao-Rui
Qu Ning
Zhou Run-Run
Wang Li-Juan
Li Shan-Hua
Li Fu-Nan
Li Hua
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Abstract
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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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KEYWORD
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Diaryl ethers, HIF-1α, p21, Cleaved caspase-3, Antitumor activity
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