Modification of 7-piperazinylquinolone antibacterials to promising anticancer lead compounds : Synthesis and in vitro studies
Copyright © 2019 Elsevier Masson SAS. All rights reserved..
Amongst the fluoroquinolone antibacterials, the 7-piperazinyl containing chemotypes such as norfloxacin, enoxacin, ciprofloxacin, pefloxacin, lomefloxacin, enrofloxacin, ofloxacin, levofloxacin, gatifloxacin and sparfloxacin have been shown to possess non-classical activities including cytotoxicity against different cancer cell lines, induction of apoptosis, and cell cycle arrest at the S/G2 stage. Additionally, piperazinylquinolones (PQs) have enough flexibility for chemical modification via their N-4 of piperazine ring and carboxylic acid at C-3. Therefore, PQs have been considered as a starting point for design and development of new anticancer agents. This review has focused on the recent synthetic modifications of PQs which led to N-substituted and/or C-3 modified PQs with potential anticancer activity.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:187 |
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| Enthalten in: |
European journal of medicinal chemistry - 187(2020) vom: 01. Feb., Seite 111970 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ahadi, Hamideh [VerfasserIn] |
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| Links: |
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| Themen: |
7-Piperazinylquinolones |
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| Anmerkungen: |
Date Completed 10.03.2020 Date Revised 10.03.2020 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2019.111970 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM304814709 |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2019 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a Amongst the fluoroquinolone antibacterials, the 7-piperazinyl containing chemotypes such as norfloxacin, enoxacin, ciprofloxacin, pefloxacin, lomefloxacin, enrofloxacin, ofloxacin, levofloxacin, gatifloxacin and sparfloxacin have been shown to possess non-classical activities including cytotoxicity against different cancer cell lines, induction of apoptosis, and cell cycle arrest at the S/G2 stage. Additionally, piperazinylquinolones (PQs) have enough flexibility for chemical modification via their N-4 of piperazine ring and carboxylic acid at C-3. Therefore, PQs have been considered as a starting point for design and development of new anticancer agents. This review has focused on the recent synthetic modifications of PQs which led to N-substituted and/or C-3 modified PQs with potential anticancer activity | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a 7-Piperazinylquinolones | |
| 650 | 4 | |a Anticancer agents | |
| 650 | 4 | |a Lead optimization | |
| 650 | 4 | |a SAR study | |
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| 650 | 7 | |a Anti-Bacterial Agents |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
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| 650 | 7 | |a Quinolones |2 NLM | |
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