New Conjugates of Daunorubicin with Sesquiterpene Lactones and Their Biological Activity
Abstract New conjugates of daunorubicin with sesquiterpene lactones at the 3′‐amino group of anthracycline were synthesized and their effect on the viability of cell lines (HL60, Jurkat, K562, and A549) was assessed using a resazurin test. The effect on the cell cycle and apoptosis by flow cytometry was studied. The following natural lactones were used for modification: telekin, isotelekin, reynosin, costunolide, dehydrocostuslactone, santamarine and epoxyisoalantolactone. The synthesized conjugates are characterized by a general high toxicity (8…0.14 μM) in relation to tumor cell lines (in some cases, higher than the toxicity of the initial antibiotic), as well as a comparable effect on the cell cycle (arrest in the G2/M‐phase) with a relatively low the effect on the initiation of apoptosis at concentrations close to the IC50..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:6 |
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| Enthalten in: |
ChemistrySelect - 6(2021), 32, Seite 8446-8451 |
| Beteiligte Personen: |
Pukhov, Sergey A. [VerfasserIn] |
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| Anmerkungen: |
© 2021 Wiley‐VCH GmbH |
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| Umfang: |
6 |
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| doi: |
10.1002/slct.202102244 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Abstract New conjugates of daunorubicin with sesquiterpene lactones at the 3′‐amino group of anthracycline were synthesized and their effect on the viability of cell lines (HL60, Jurkat, K562, and A549) was assessed using a resazurin test. The effect on the cell cycle and apoptosis by flow cytometry was studied. The following natural lactones were used for modification: telekin, isotelekin, reynosin, costunolide, dehydrocostuslactone, santamarine and epoxyisoalantolactone. The synthesized conjugates are characterized by a general high toxicity (8…0.14 μM) in relation to tumor cell lines (in some cases, higher than the toxicity of the initial antibiotic), as well as a comparable effect on the cell cycle (arrest in the G2/M‐phase) with a relatively low the effect on the initiation of apoptosis at concentrations close to the IC50. | ||
| 700 | 1 | |a Semakov, Alexey V. |4 aut | |
| 700 | 1 | |a Globa, Anastasiya A. |4 aut | |
| 700 | 1 | |a Anikina, Lada V. |4 aut | |
| 700 | 1 | |a Afanasyeva, Svetlana V. |4 aut | |
| 700 | 1 | |a Yandulova, Ekaterina Y. |4 aut | |
| 700 | 1 | |a Aleksandrova, Yulia R. |4 aut | |
| 700 | 1 | |a Neganova, Margarita E. |4 aut | |
| 700 | 1 | |a Klochkov, Sergey G. |4 aut | |
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