Synthesis, anticancer activity, structure-activity relationship and binding mode of interaction studies of substituted pentanoic acids
Aim: Simultaneous inhibition of MMP-2 and HDAC8 may be an effective strategy to target cancer. Methodology: In continuation of our earlier efforts, a series of substituted pentanoic acids (1-18) were synthesized and checked for their biological activity along with some earlier reported compounds (19-35). Results: Compounds 18 and 31 were found to induce apoptosis effectively in a dose-dependent fashion in Jurkat-E6.1 cell line. They reduced the expression of both MMP-2 and HDAC8 effectively. 31 also produced prominent intensity of fluorescence to bring nick in Jurkat-E6.1 cells. 31 also showed cellular arrest in sub-G0 phase. Conclusion: Such compounds may be useful to battle against cancer.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 14 vom: 28. Juli, Seite 1679-1702 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Dutta, Sanchita [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 01.06.2020 Date Revised 01.06.2020 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2018-0361 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM299820874 |
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| 245 | 1 | 0 | |a Synthesis, anticancer activity, structure-activity relationship and binding mode of interaction studies of substituted pentanoic acids |
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| 500 | |a Date Completed 01.06.2020 | ||
| 500 | |a Date Revised 01.06.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Simultaneous inhibition of MMP-2 and HDAC8 may be an effective strategy to target cancer. Methodology: In continuation of our earlier efforts, a series of substituted pentanoic acids (1-18) were synthesized and checked for their biological activity along with some earlier reported compounds (19-35). Results: Compounds 18 and 31 were found to induce apoptosis effectively in a dose-dependent fashion in Jurkat-E6.1 cell line. They reduced the expression of both MMP-2 and HDAC8 effectively. 31 also produced prominent intensity of fluorescence to bring nick in Jurkat-E6.1 cells. 31 also showed cellular arrest in sub-G0 phase. Conclusion: Such compounds may be useful to battle against cancer | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a SAR | |
| 650 | 4 | |a apoptosis | |
| 650 | 4 | |a cell cycle | |
| 650 | 4 | |a cytotoxicity | |
| 650 | 4 | |a flow cytometry | |
| 650 | 4 | |a leukemia | |
| 650 | 4 | |a metalloenzyme | |
| 650 | 4 | |a mitochondrial membrane potential | |
| 650 | 4 | |a molecular docking | |
| 650 | 4 | |a pentanoic acid | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Pentanoic Acids |2 NLM | |
| 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 Saha, Achintya |e verfasserin |4 aut | |
| 700 | 1 | |a Jha, Tarun |e verfasserin |4 aut | |
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