Synthesis, anticancer activity, SAR and binding mode of interaction studies of substituted pentanoic acids : part II
Aim: Our previous results suggest that phenyl/naphthylacetyl pentanoic acid derivatives may exhibit dual MMP-2 and HDAC8 inhibitory activities and show effective cytotoxic properties. Methodology: Here, 13 new compounds (C1-C13) were synthesized and characterized. Along with these new compounds, 16 previously reported phenyl/napthylacetyl pentanoic acid derivatives (C14-C29) were biologically evaluated. Results: Compounds C6 and C27 showed good cytotoxicity against leukemia cell line Jurkat E6.1. The mechanisms of cytotoxicity of these compounds were confirmed by DNA deformation assay and reactive oxygen species assay. MMP-2 and HDAC8 expression assays suggested the dual inhibiting property of these two compounds. These findings were supported by results of molecular docking studies. In silico pharmacokinetic properties showed compounds C6 and C27 have high gastrointestinal absorption. Conclusion: This study highlights the action of phenyl/naphthylacetyl pentanoic acid derivatives as anticancer agents.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
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| Enthalten in: |
Future medicinal chemistry - 14(2022), 1 vom: 08. Jan., Seite 17-34 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Datta, Sanchita [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 10.02.2022 Date Revised 10.02.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2021-0049 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM333561058 |
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| 100 | 1 | |a Datta, Sanchita |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Synthesis, anticancer activity, SAR and binding mode of interaction studies of substituted pentanoic acids |b part II |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Our previous results suggest that phenyl/naphthylacetyl pentanoic acid derivatives may exhibit dual MMP-2 and HDAC8 inhibitory activities and show effective cytotoxic properties. Methodology: Here, 13 new compounds (C1-C13) were synthesized and characterized. Along with these new compounds, 16 previously reported phenyl/napthylacetyl pentanoic acid derivatives (C14-C29) were biologically evaluated. Results: Compounds C6 and C27 showed good cytotoxicity against leukemia cell line Jurkat E6.1. The mechanisms of cytotoxicity of these compounds were confirmed by DNA deformation assay and reactive oxygen species assay. MMP-2 and HDAC8 expression assays suggested the dual inhibiting property of these two compounds. These findings were supported by results of molecular docking studies. In silico pharmacokinetic properties showed compounds C6 and C27 have high gastrointestinal absorption. Conclusion: This study highlights the action of phenyl/naphthylacetyl pentanoic acid derivatives as anticancer agents | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 7 | |a Pentanoic Acids |2 NLM | |
| 650 | 7 | |a Reactive Oxygen Species |2 NLM | |
| 650 | 7 | |a Repressor Proteins |2 NLM | |
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| 700 | 1 | |a Halder, Amit Kumar |e verfasserin |4 aut | |
| 700 | 1 | |a Adhikari, Nilanjan |e verfasserin |4 aut | |
| 700 | 1 | |a Amin, Sk Abdul |e verfasserin |4 aut | |
| 700 | 1 | |a Das, Sanjib |e verfasserin |4 aut | |
| 700 | 1 | |a Jha, Tarun |e verfasserin |4 aut | |
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