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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
In search of a cytostatic agent derived from the alkaloid lycorine: Synthesis and growth inhibitory properties of lycorine derivatives
Bioorganic and Medicinal Chemistry, Volume 19, No. 23, Year 2011
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Description
As a continuation of our studies aimed at the development of a new cytostatic agent derived from an Amaryllidaceae alkaloid lycorine, we synthesized 32 analogues of this natural product. This set of synthetic analogues included compounds incorporating selective derivatization of the C1 versus C2 hydroxyl groups, aromatized ring C, lactamized N6 nitrogen, dihydroxylated C3-C3a olefin functionality, transposed olefin from C3-C3a to C2-C3 or C3a-C4, and C1 long-chain fatty esters. All synthesized compounds were evaluated for antiproliferative activities in vitro in a panel of tumor cell lines including those exhibiting resistance to proapoptotic stimuli and representing solid cancers associated with dismal prognoses, such as melanoma, glioblastoma, and non-small-cell lung cancer. Most active analogues were not discriminatory between cancer cells displaying resistance or sensitivity to apoptosis, indicating that these compounds are thus able to overcome the intrinsic resistance of cancer cells to pro-apoptotic stimuli. 1,2-Di-O-allyllycorine was identified as a lycorine analogue, which is 100 times more potent against a U373 human glioblastoma model than the parent natural product. Furthermore, a number of synthetic analogues were identified as promising for the forthcoming in vivo studies. © 2011 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Evdokimov, Nikolai M.
United States, Socorro
New Mexico Institute of Mining and Technology
Lamoral-Theys, Delphine
Belgium, Brussels
Laboratoire de Chimie Analytique
Mathieu, Véronique
Belgium, Brussels
Université Libre de Bruxelles
Andolfi, Anna
Italy, Naples
Università Degli Studi Di Napoli Federico Ii
Frolova, Liliya V.
United States, Socorro
New Mexico Institute of Mining and Technology
Pelly, Stephen C.
South Africa, Stellenbosch
Stellenbosch University
van Otterlo, Willem A. L.
South Africa, Stellenbosch
Stellenbosch University
Magedov, Igor V.
United States, Socorro
New Mexico Institute of Mining and Technology
Kiss, Robert
Belgium, Brussels
Université Libre de Bruxelles
Evidente, Antonio
Italy, Naples
Università Degli Studi Di Napoli Federico Ii
Kornienko, Alexander V.
United States, Socorro
New Mexico Institute of Mining and Technology
Statistics
Citations: 47
Authors: 11
Affiliations: 5
Identifiers
Doi:
10.1016/j.bmc.2011.09.051
ISSN:
09680896
e-ISSN:
14643391
Research Areas
Cancer