Synthesis and structure-activity relationship of N-(piperidin-4-yl)benzamide derivatives as activators of hypoxia-inducible factor 1 pathways

Archives of Pharmacal Research
Zhi-Ning HuangFu-Nan Li

Abstract

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.

References

Nov 21, 2007·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·M Christiane Brahimi-HornJacques Pouysségur
Feb 9, 2008·Cell Death and Differentiation·E B Rankin, A J Giaccia
Jun 4, 2010·Nature·Ataman SendoelMichael O Hengartner
Oct 23, 2010·Molecular Cell·Amar J MajmundarM Celeste Simon
Dec 6, 2012·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Hai-Xiang SunJia Fan

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Citations

Dec 29, 2020·Bioorganic & Medicinal Chemistry·Semih YagciGokcen Eren

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