Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 25, Issue 13, Pages 3357-3367Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.04.021
Keywords
Artemisinin; Cholic acid; Artemisin-derived hybrid; Leukemia; Anticancer activity
Funding
- Bodossaki Foundation (Vasileos Georgiou B' 5, Athens, Greece)
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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 0.019 M-0.192 M against CCRF-CEM cells and between 0.345 JAM and 7.159 M 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 +/- 0.001 mu M and 0.345 +/- 0.031 mu M, 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. (C) 2017 Elsevier Ltd. All rights reserved.
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