Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 12, Pages 3610-3618Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.05.041
Keywords
Natural product hybrid; Artemisinin; Thymoquinone; Egonol; Antileukemia activity; Antimalarial activity; Antiviral activity
Funding
- Deutsche Forschungsgemeinschaft (DFG) [TS 87/16-3, MA 1289/7-3]
- Emerging Fields Initiative (EFI) Chemistry in Live Cells - Friedrich-Alexander-Universitat Erlangen-Nurnberg
- Interdisciplinary Center for Molecular Materials (ICMM)
- Graduate School Molecular Science (GSMS)
- German Academic Exchange Service DAAD
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Hybridization of natural products has high potential to further improve their activities and may produce synergistic effects between linked pharmacophores. Here we report synthesis of nine new hybrids of natural products egonol, homoegonol, thymoquinone and artemisinin and evaluation of their activities against P. falciparum 3D7 parasites, human cytomegalovirus, sensitive and multidrug-resistant human leukemia cells. Most of the new hybrids exceed their parent compounds in antimalarial, antiviral and antileukemia activities and in some cases show higher in vitro efficacy than clinically used reference drugs chloroquine, ganciclovir and doxorubicin. Combined, our findings stress the high potency of these hybrids and encourages further use of the hybridization concept in applied pharmacological research.
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