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Epoxides related to dioncoquinone B: Synthesis, activity against multiple myeloma cells, and search for the target protein

Abstract:

Epoxide 2b is an analog of the synthetic intermediate 2a en route to the polyketide-derived antitumoral naphthoquinone dioncoquinone B (1), isolated from cell cultures of the tropical liana Triphyophyllum peltatum (Dioncophyllaceae). Compound 2b was found to induce strong apoptosis in multiple myeloma cells at a concentration (EC50 = 3.5 μM), distinctly lower than that of 1 and any related analog, without exerting significant toxicity against normal blood cells. Preliminary studies showed tha...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.tet.2018.04.056

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
NDM; Target Discovery Institute
Feineis, D More by this author
Brünnert, D More by this author
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Publisher:
Elsevier Publisher's website
Journal:
Tetrahedron Journal website
Volume:
74
Issue:
38
Pages:
5102-5112
Publication date:
2018-04-19
Acceptance date:
2018-04-17
DOI:
EISSN:
1464-5416
ISSN:
0040-4020
Pubs id:
pubs:864001
URN:
uri:455079d8-017f-478e-9c36-443d04bfa810
UUID:
uuid:455079d8-017f-478e-9c36-443d04bfa810
Local pid:
pubs:864001

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