Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells

Publication type:
Journal article
Metadata:
Autoren
  • Antonios S Letis
  • Ean-Jeong Seo
  • Sotiris S Nikolaropoulos
  • Thomas Efferth
  • Athanassios Giannis
  • Manolis A Fousteris
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000402941700008&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1016/j.bmc.2017.04.021
eISSN
1464-3391
Externe Identifier
  • Clarivate Analytics Document Solution ID: EX0WO
  • PubMed Identifier: 28456567
ISSN
0968-0896
Ausgabe der Veröffentlichung
13
Zeitschrift
BIOORGANIC & MEDICINAL CHEMISTRY
Schlüsselwörter
  • Artemisinin
  • Cholic acid
  • Artemisin-derived hybrid
  • Leukemia
  • Anticancer activity
Paginierung
3357 - 3367
Datum der Veröffentlichung
2017
Status
Published
Titel
Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells
Sub types
  • Article
Ausgabe der Zeitschrift
25

Data source: Web of Science (Lite)

Other metadata sources:
Autoren
  • Antonios S Letis
  • Ean-Jeong Seo
  • Sotiris S Nikolaropoulos
  • Thomas Efferth
  • Athanassios Giannis
  • Manolis A Fousteris
DOI
10.1016/j.bmc.2017.04.021
ISSN
0968-0896
Ausgabe der Veröffentlichung
13
Zeitschrift
Bioorganic & Medicinal Chemistry
Sprache
en
Paginierung
3357 - 3367
Datum der Veröffentlichung
2017
Status
Published
Herausgeber
Elsevier BV
Herausgeber URL
http://dx.doi.org/10.1016/j.bmc.2017.04.021
Datum der Datenerfassung
2022
Titel
Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells
Ausgabe der Zeitschrift
25

Data source: Crossref

Abstract
A series of new artemisinin-derived hybrids which incorporate cholic acid moieties have been synthesized and evaluated for their antileukemic activity against sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells. The new hybrids 20-28 showed IC<sub>50</sub> values in the range of 0.019µM-0.192µM against CCRF-CEM cells and between 0.345µM and 7.159µM against CEM/ADR5000 cells. Amide hybrid 25 proved the most active compound against both CCRF-CEM and CEM/ADR5000 cells with IC<sub>50</sub> value of 0.019±0.001µM and 0.345±0.031µM, respectively. A relatively low cross resistance to hybrids 20-28 in the range of 5.7-fold to 46.1-fold was measured. CEM/ADR5000 cells showed higher resistance than CCRF-CEM to all the tested compounds. Interestingly, the lowest cross resistance to 23 was observed (5.7-fold), whereas hybrid 25 showed 18.2-fold cross-resistant to CEM/ADR5000 cells. Hybrid 25 which proved even more potent than clinically used doxorubicin against CEM/ADR5000 cells may serve as a promising antileukemic agent against both sensitive and multidrug-resistant cells.
Addresses
  • Laboratory of Medicinal Chemistry, Department of Pharmacy, University of Patras, Patras GR-26500, Greece.
Autoren
  • Antonios S Letis
  • Ean-Jeong Seo
  • Sotiris S Nikolaropoulos
  • Thomas Efferth
  • Thomas Efferth
  • Athanassios Giannis
  • Manolis A Fousteris
DOI
10.1016/j.bmc.2017.04.021
eISSN
1464-3391
Externe Identifier
  • PubMed Identifier: 28456567
Funding acknowledgements
  • Bodossaki Foundation:
Open access
false
ISSN
0968-0896
Ausgabe der Veröffentlichung
13
Zeitschrift
Bioorganic & medicinal chemistry
Schlüsselwörter
  • Tumor Cells, Cultured
  • Humans
  • Leukemia
  • Artemisinins
  • Antineoplastic Agents
  • Drug Screening Assays, Antitumor
  • Cell Proliferation
  • Molecular Structure
  • Structure-Activity Relationship
  • Dose-Response Relationship, Drug
Sprache
eng
Medium
Print-Electronic
Online publication date
2017
Paginierung
3357 - 3367
Datum der Veröffentlichung
2017
Status
Published
Datum der Datenerfassung
2017
Titel
Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells.
Sub types
  • Journal Article
Ausgabe der Zeitschrift
25

Data source: Europe PubMed Central

Abstract
A series of new artemisinin-derived hybrids which incorporate cholic acid moieties have been synthesized and evaluated for their antileukemic activity against sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells. The new hybrids 20-28 showed IC50 values in the range of 0.019µM-0.192µM against CCRF-CEM cells and between 0.345µM and 7.159µM against CEM/ADR5000 cells. Amide hybrid 25 proved the most active compound against both CCRF-CEM and CEM/ADR5000 cells with IC50 value of 0.019±0.001µM and 0.345±0.031µM, respectively. A relatively low cross resistance to hybrids 20-28 in the range of 5.7-fold to 46.1-fold was measured. CEM/ADR5000 cells showed higher resistance than CCRF-CEM to all the tested compounds. Interestingly, the lowest cross resistance to 23 was observed (5.7-fold), whereas hybrid 25 showed 18.2-fold cross-resistant to CEM/ADR5000 cells. Hybrid 25 which proved even more potent than clinically used doxorubicin against CEM/ADR5000 cells may serve as a promising antileukemic agent against both sensitive and multidrug-resistant cells.
Date of acceptance
2017
Autoren
  • Antonios S Letis
  • Ean-Jeong Seo
  • Sotiris S Nikolaropoulos
  • Thomas Efferth
  • Athanassios Giannis
  • Manolis A Fousteris
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/28456567
DOI
10.1016/j.bmc.2017.04.021
eISSN
1464-3391
Ausgabe der Veröffentlichung
13
Zeitschrift
Bioorg Med Chem
Schlüsselwörter
  • Anticancer activity
  • Artemisin-derived hybrid
  • Artemisinin
  • Cholic acid
  • Leukemia
  • Antineoplastic Agents
  • Artemisinins
  • Cell Proliferation
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Leukemia
  • Molecular Structure
  • Structure-Activity Relationship
  • Tumor Cells, Cultured
Sprache
eng
Country
England
Paginierung
3357 - 3367
PII
S0968-0896(17)30542-4
Datum der Veröffentlichung
2017
Status
Published
Datum, an dem der Datensatz öffentlich gemacht wurde
2017
Titel
Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells.
Sub types
  • Journal Article
Ausgabe der Zeitschrift
25

Data source: PubMed

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