Anti-cancer activity of carbamate derivatives of melampomagnolide B |
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Affiliation: | 1. Department of Cardiology, Fukuoka University School of Medicine, Japan;2. The AIG Collaborative Research Institute of Cardiovascular Medicine, Japan;3. Department of Chemistry, Faculty of Science, Fukuoka University, Fukuoka, Japan;1. cE3c-Centre for Ecology, Evolution and Environmental Changes/Azorean Biodiversity Group & Faculty of Sciences and Technology, University of Azores, Rua Mãe de Deus, Ponta Delgada, Portugal |
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Abstract: | Melampomagnolide B (MMB) is a natural sesquiterpene structurally related to parthenolide (PTL). We have shown that MMB exhibits anti-leukemic properties similar to PTL. Unlike PTL, the presence of a primary hydroxyl group in the MMB molecule allows the opportunity for examining the biological activity of a variety of conjugated analogs of MMB. We have now synthesized a series of carbamate analogs of MMB and evaluated these derivatives for anti-cancer activity against a panel of sixty human cancer cell lines. Analogs 6a and 6e exhibited promising anti-leukemic activity against human leukemia cell line CCRF-CEM with GI50 values of 680 and 620 nM, respectively. Analog 6a also showed GI50 values of 1.98 and 1.38 μM respectively, against RPMI-8226 and SR leukemia cell lines and GI50 values of 460 and 570 nM against MDA-MB-435 melanoma and MDA-MB-468 breast cancer cell lines, respectively. Analog 6e had GI50 values of 650 and 900 nM against HOP-92 non-small cell lung and RXF 393 renal cancer cell lines. |
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Keywords: | Parthenolide Melampomagnolide B Anti-cancer activity Carbamates Heterocyclic amines |
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