Antimelanoma activities of chimeric thiazole-androstenone derivatives
© 2021 The Authors..
The discovery of chimeric anti-melanoma agents is reported. These molecules are potent growth suppressors of melanoma cells in vitro with growth inhibition of 50% (GI50) values as low as 1.32 µM. Compounds were more toxic to melanoma cells in vitro than commonly used anti-melanoma agent dacarbazine as measured by TUNEL assay. They induced both caspase-independent apoptosis evident by colocalization of TUNEL with endonuclease G (EndoG) and caspase-mediated apoptosis measured by colocalization of TUNEL with caspase-activated DNase (CAD). In addition, compounds 3 and 5 strongly induced oxidative injury to melanoma cells as measured by TUNEL colocalization with heme oxygenase-1 (HO1). Dacarbazine induced only caspase-independent apoptosis, which may explain why it is less cytotoxic to melanoma cells than compounds 3, 4 and 5.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:8 |
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| Enthalten in: |
Royal Society open science - 8(2021), 8 vom: 01. Aug., Seite 210395 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chambers, Steven A [VerfasserIn] |
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| Links: |
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| Themen: |
Androstenone |
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| Anmerkungen: |
Date Revised 26.08.2021 published: Electronic-eCollection figshare: 10.6084/m9.figshare.c.5542597 Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1098/rsos.210395 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a The discovery of chimeric anti-melanoma agents is reported. These molecules are potent growth suppressors of melanoma cells in vitro with growth inhibition of 50% (GI50) values as low as 1.32 µM. Compounds were more toxic to melanoma cells in vitro than commonly used anti-melanoma agent dacarbazine as measured by TUNEL assay. They induced both caspase-independent apoptosis evident by colocalization of TUNEL with endonuclease G (EndoG) and caspase-mediated apoptosis measured by colocalization of TUNEL with caspase-activated DNase (CAD). In addition, compounds 3 and 5 strongly induced oxidative injury to melanoma cells as measured by TUNEL colocalization with heme oxygenase-1 (HO1). Dacarbazine induced only caspase-independent apoptosis, which may explain why it is less cytotoxic to melanoma cells than compounds 3, 4 and 5 | ||
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| 700 | 1 | |a Basnakian, Alexei G |e verfasserin |4 aut | |
| 700 | 1 | |a Alam, Mohammad A |e verfasserin |4 aut | |
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