Synthesis and structure–activity relationship of N-(piperidin-4-yl)benzamide derivatives as activators of hypoxia-inducible factor 1 pathways
| Autor: | Run-Run Zhou, Li Shanhua, Liang Han, Ning Qu, Fu-Nan Li, Wang Baorui, Hong Qiao, Zhi-Ning Huang, Hua Li, Li-Juan Wang |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Hypoxia-Inducible Factor 1 Antineoplastic Agents Apoptosis Caspase 3 Inhibitory postsynaptic potential Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Downregulation and upregulation Drug Discovery Humans Structure–activity relationship Benzamide Cell Proliferation Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Hep G2 Cells Hypoxia-Inducible Factor 1 alpha Subunit In vitro 030104 developmental biology Biochemistry Benzamides Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Archives of Pharmacal Research. 41:1149-1161 |
| ISSN: | 1976-3786 0253-6269 |
| DOI: | 10.1007/s12272-018-1050-2 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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