Design and synthesis of β-carboline linked aryl sulfonyl piperazine derivatives : DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability
Copyright © 2020 Elsevier Inc. All rights reserved..
A series of new β-carboline linked aryl sulfonyl piperazine congeners have been synthesized by coupling various β-carboline acids with substituted aryl sulfonyl piperazines. Evaluation of their anticancer activity against a panel of human cancer cell lines such as colon (HT-29), breast (MDA-MB-231), bone osteosarcoma (MG-63), brain (U87 MG), prostate (PC- 3) and normal monkey kidney (Vero) cell line has been done. Among the series, compound 8ec and 8ed has shown most potent cytotoxicity with an IC50 values of 2.80 ± 0.10 µM and 0.59 ± 0.28 µM respectively against MG-63 cell line and also potent on other cell lines tested. Compounds 8ec and 8ed was found to inhibit Topo II that is confirmed by specific Topo II inhibition assay. DNA binding studies, cell cycle analysis, Annexin V study indicate that these compounds has potential anticancer activity. Molecular docking studies for compound 8ec and 8ed are incorporated to understand the nature of interaction with topoisomerase IIα and dsDNA.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:101 |
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| Enthalten in: |
Bioorganic chemistry - 101(2020) vom: 02. Aug., Seite 103983 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Lakshmi Manasa, Kesari [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 02.03.2021 Date Revised 02.03.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bioorg.2020.103983 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM312594569 |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2020 Elsevier Inc. All rights reserved. | ||
| 520 | |a A series of new β-carboline linked aryl sulfonyl piperazine congeners have been synthesized by coupling various β-carboline acids with substituted aryl sulfonyl piperazines. Evaluation of their anticancer activity against a panel of human cancer cell lines such as colon (HT-29), breast (MDA-MB-231), bone osteosarcoma (MG-63), brain (U87 MG), prostate (PC- 3) and normal monkey kidney (Vero) cell line has been done. Among the series, compound 8ec and 8ed has shown most potent cytotoxicity with an IC50 values of 2.80 ± 0.10 µM and 0.59 ± 0.28 µM respectively against MG-63 cell line and also potent on other cell lines tested. Compounds 8ec and 8ed was found to inhibit Topo II that is confirmed by specific Topo II inhibition assay. DNA binding studies, cell cycle analysis, Annexin V study indicate that these compounds has potential anticancer activity. Molecular docking studies for compound 8ec and 8ed are incorporated to understand the nature of interaction with topoisomerase IIα and dsDNA | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Aryl sulfonyl piperazine | |
| 650 | 4 | |a Cytotoxicity and Molecular docking | |
| 650 | 4 | |a DNA binding studies | |
| 650 | 4 | |a Topoisomerase II inhibition | |
| 650 | 4 | |a β-carboline | |
| 650 | 7 | |a Carbolines |2 NLM | |
| 650 | 7 | |a Topoisomerase II Inhibitors |2 NLM | |
| 700 | 1 | |a Thatikonda, Sowjanya |e verfasserin |4 aut | |
| 700 | 1 | |a Sigalapalli, Dilep Kumar |e verfasserin |4 aut | |
| 700 | 1 | |a Sagar, Arpita |e verfasserin |4 aut | |
| 700 | 1 | |a Kiranmai, Gaddam |e verfasserin |4 aut | |
| 700 | 1 | |a Kalle, Arunasree M |e verfasserin |4 aut | |
| 700 | 1 | |a Alvala, Mallika |e verfasserin |4 aut | |
| 700 | 1 | |a Godugu, Chandraiah |e verfasserin |4 aut | |
| 700 | 1 | |a Nagesh, Narayana |e verfasserin |4 aut | |
| 700 | 1 | |a Nagendra Babu, Bathini |e verfasserin |4 aut | |
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