Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin

Capci Karagöz A, Reiter C, Seo EJ, Gruber L, Hahn F, Leidenberger M, Klein V, Hampel F, Friedrich O, Marschall M, Kappes B, Efferth T, Tsogoeva S (2018)

Publication Type: Journal article

Publication year: 2018

Journal

Bioorganic & Medicinal Chemistry Elsevier

Book Volume: 26

Pages Range: 3610-3618

Journal Issue: 12

DOI: 10.1016/j.bmc.2018.05.041

Abstract

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.

Authors with CRIS profile

Aysun Capci Karagöz Professur für Organische Chemie Friedrich Hahn Professur für Virologie Maria Leidenberger Lehrstuhl für Medizinische Biotechnologie Volker Klein Lehrstuhl für Organische Chemie I Frank Hampel Lehrstuhl für Organische Chemie I Oliver Friedrich Lehrstuhl für Medizinische Biotechnologie Manfred Marschall Lehrstuhl für Klinische und Molekulare Virologie Bärbel Kappes Lehrstuhl für Medizinische Biotechnologie Svetlana Tsogoeva Professur für Organische Chemie

Involved external institutions

Johannes Gutenberg-Universität Mainz (JGU) DE Germany (DE)

How to cite

APA:

Capci Karagöz, A., Reiter, C., Seo, E.-J., Gruber, L., Hahn, F., Leidenberger, M.,... Tsogoeva, S. (2018). Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin. Bioorganic & Medicinal Chemistry, 26(12), 3610-3618. https://dx.doi.org/10.1016/j.bmc.2018.05.041

MLA:

Capci Karagöz, Aysun, et al. "Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin." Bioorganic & Medicinal Chemistry 26.12 (2018): 3610-3618.

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