Exploring the N1 Position of Biginelli Compounds : New Insights and Trends for Chemical Diversity Generation of Bioactive Derivatives
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
Dihydropyrimidinones (DHPMs) are heterocycles obtained by the multicomponent Biginelli reaction. Recently, new synthetic protocols have allowed us to explore functionalisation at less explored positions of DHPMs, such as the N1 position. In this context, a full literature survey of N1- substituted DHPMs was performed. We analysed 27 papers and identified 379 compounds with substituents at the N1 position, most of them with alkyl groups, and a total of 28% compounds with aromatic substituents attached at the N1 position. N1-substituted DHPMs were explored mainly due to their effects on cancer cell proliferation via numerous targets, such as kinesin Eg5, heat shock protein 70, heat shock protein 90, and the epidermal growth factor receptor. Similarity analyses were performed using the data of 379 DHPMs from different cheminformatic approaches, i.e., chemical property correlations, principal component analysis, similarity networks, and compound clustering.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:22 |
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| Enthalten in: |
Mini reviews in medicinal chemistry - 22(2022), 11 vom: 08., Seite 1545-1558 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Gonçalves, Itamar Luís [VerfasserIn] |
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| Links: |
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| Themen: |
Biginelli reactions |
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| Anmerkungen: |
Date Completed 29.07.2022 Date Revised 29.07.2022 published: Print Citation Status MEDLINE |
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| doi: |
10.2174/1389557521666211027105534 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net. | ||
| 520 | |a Dihydropyrimidinones (DHPMs) are heterocycles obtained by the multicomponent Biginelli reaction. Recently, new synthetic protocols have allowed us to explore functionalisation at less explored positions of DHPMs, such as the N1 position. In this context, a full literature survey of N1- substituted DHPMs was performed. We analysed 27 papers and identified 379 compounds with substituents at the N1 position, most of them with alkyl groups, and a total of 28% compounds with aromatic substituents attached at the N1 position. N1-substituted DHPMs were explored mainly due to their effects on cancer cell proliferation via numerous targets, such as kinesin Eg5, heat shock protein 70, heat shock protein 90, and the epidermal growth factor receptor. Similarity analyses were performed using the data of 379 DHPMs from different cheminformatic approaches, i.e., chemical property correlations, principal component analysis, similarity networks, and compound clustering | ||
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| 650 | 4 | |a DHPMs | |
| 650 | 4 | |a Multicomponent reactions | |
| 650 | 4 | |a bioactive derivatives | |
| 650 | 4 | |a molecular diversity | |
| 650 | 4 | |a privileged structure | |
| 650 | 7 | |a Pyrimidinones |2 NLM | |
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| 700 | 1 | |a Kagami, Luciano Porto |e verfasserin |4 aut | |
| 700 | 1 | |a Gonçalves, Guilherme Arraché |e verfasserin |4 aut | |
| 700 | 1 | |a Davi, Leonardo |e verfasserin |4 aut | |
| 700 | 1 | |a Eifler-Lima, Vera Lucia |e verfasserin |4 aut | |
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