Synthesis, anticancer activity, SAR and binding mode of interaction studies of substituted pentanoic acids: part II / Sanchita Datta, Amit Kumar Halder, Nilanjan Adhikari, Sk Abdul Amin, Sanjib Das, Tarun Jha
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:CompoundsC6andC27showed 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 silicopharmacokinetic properties showed compoundsC6andC27have high gastrointestinal absorption.Conclusion:This study highlights the action of phenyl/naphthylacetyl pentanoic acid derivatives as anticancer agents. Aim: Methodology: C1–C13 C14–C29 Results: C6 C27 In silico C6 C27 Conclusion.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
Erscheinungsort nicht ermittelbar: 2021 |
| Enthalten in: |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
Datta, Sanchita [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Themen: |
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| Umfang: |
1 Online-Ressource (18 p) |
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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): |
KFL011093757 |
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| 245 | 1 | 0 | |a Synthesis, anticancer activity, SAR and binding mode of interaction studies of substituted pentanoic acids: part II |c Sanchita Datta, Amit Kumar Halder, Nilanjan Adhikari, Sk Abdul Amin, Sanjib Das, Tarun Jha |
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| 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:CompoundsC6andC27showed 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 silicopharmacokinetic properties showed compoundsC6andC27have high gastrointestinal absorption.Conclusion:This study highlights the action of phenyl/naphthylacetyl pentanoic acid derivatives as anticancer agents. Aim: Methodology: C1–C13 C14–C29 Results: C6 C27 In silico C6 C27 Conclusion | ||
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| 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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