New pharmacological findings linked to biphenyl DHPMs, kinesin Eg5 ligands : anticancer and antioxidant effects
Background: Dihydropyrimidin-2-thiones (DHPMs) are a class of heterocyclic compound which have been intensively investigated mainly due to their anticancer activity as kinesin Eg5 inhibitors. Materials & methods: A library of N1 aryl substituted DHPMs were tested against glioma and bladder cancer cell lines. Quantitative structure-activity relationship (QSAR) investigation was performed in order to identify key elements of DHPMs linked with their antiproliferative effect. The toxicity of most active compounds was investigated using Caenorhabditis elegans as the model. Results & conclusion: DHPMs 9, 13 and 17 have been identified as having improved activity against glioma and bladder cell lines as compared with monastrol. Flow cytometry investigations showed that the new compounds induce cell cycle arrest in phase G2/M and cell death by apoptosis. In addition, compound 13 was able to modulate the reactive oxygen species production in vivo in C. elegans. The biphenyl dihydropyrimidinthiones provided a safety profile in C. elegans.
| Errataetall: |
ErratumIn: Future Med Chem. 2020 Sep;12(18):1685. - PMID 32842787 |
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| Medienart: |
E-Artikel |
| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Future medicinal chemistry - 12(2020), 12 vom: 07. Juni, Seite 1137-1154 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Gonçalves, Itamar Luís [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 21.05.2021 Date Revised 04.12.2021 published: Print-Electronic ErratumIn: Future Med Chem. 2020 Sep;12(18):1685. - PMID 32842787 Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2019-0256 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM310924901 |
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| 245 | 1 | 0 | |a New pharmacological findings linked to biphenyl DHPMs, kinesin Eg5 ligands |b anticancer and antioxidant effects |
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| 520 | |a Background: Dihydropyrimidin-2-thiones (DHPMs) are a class of heterocyclic compound which have been intensively investigated mainly due to their anticancer activity as kinesin Eg5 inhibitors. Materials & methods: A library of N1 aryl substituted DHPMs were tested against glioma and bladder cancer cell lines. Quantitative structure-activity relationship (QSAR) investigation was performed in order to identify key elements of DHPMs linked with their antiproliferative effect. The toxicity of most active compounds was investigated using Caenorhabditis elegans as the model. Results & conclusion: DHPMs 9, 13 and 17 have been identified as having improved activity against glioma and bladder cell lines as compared with monastrol. Flow cytometry investigations showed that the new compounds induce cell cycle arrest in phase G2/M and cell death by apoptosis. In addition, compound 13 was able to modulate the reactive oxygen species production in vivo in C. elegans. The biphenyl dihydropyrimidinthiones provided a safety profile in C. elegans | ||
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| 700 | 1 | |a Eifler-Lima, Vera Lucia |e verfasserin |4 aut | |
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