Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines
Copyright © 2024 Elsevier Ltd. All rights reserved..
A structure-activity relationship study performed on 1H-pyrrolo[3,2-g]isoquinoline scaffold identified new haspin inhibitors with nanomolar potencies and selectivity indices (SI) over 6 (inhibitory potency evaluated against 8 protein kinases). Compound 22 was the most active of the series (haspin IC50 = 76 nM). Cellular evaluation of 22 confirmed its activity for endogenous haspin in U-2 OS cells and its anti-proliferative activity against various cell lines. In addition, the binding mode of analog 22 in complex with haspin was determined by X-ray crystallography.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:100 |
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| Enthalten in: |
Bioorganic & medicinal chemistry - 100(2024) vom: 15. Feb., Seite 117619 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Defois, Mathilde [VerfasserIn] |
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| Links: |
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| Themen: |
Cellular activity |
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| Anmerkungen: |
Date Completed 23.02.2024 Date Revised 23.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmc.2024.117619 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a A structure-activity relationship study performed on 1H-pyrrolo[3,2-g]isoquinoline scaffold identified new haspin inhibitors with nanomolar potencies and selectivity indices (SI) over 6 (inhibitory potency evaluated against 8 protein kinases). Compound 22 was the most active of the series (haspin IC50 = 76 nM). Cellular evaluation of 22 confirmed its activity for endogenous haspin in U-2 OS cells and its anti-proliferative activity against various cell lines. In addition, the binding mode of analog 22 in complex with haspin was determined by X-ray crystallography | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Knapp, Stefan |e verfasserin |4 aut | |
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| 700 | 1 | |a Ruchaud, Sandrine |e verfasserin |4 aut | |
| 700 | 1 | |a Moreau, Pascale |e verfasserin |4 aut | |
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