- First total synthesis of protoapigenone and its analogues as potent cytotoxic agents
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Protoapigenone (1), isolated from Thelypteris torresiana, previously showed significant cytotoxic activity against five human cancer cell lines. In a continued structure-activity relationship study, the first total synthesis and modification of 1 were ach
- Lin, An-Shen,Nakagawa-Goto, Kyoko,Chang, Fang-Rong,Yu, Donglei,Morris-Natschke, Susan L.,Wu, Chin-Chung,Chen, Shu-Li,Wu, Yang-Chang,Lee, Kuo-Hsiung
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- Synthesis and SAR Study of Anticancer Protoflavone Derivatives: Investigation of Cytotoxicity and Interaction with ABCB1 and ABCG2 Multidrug Efflux Transporters
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There is a constant need for new therapies against multidrug-resistant (MDR) cancer. Natural compounds are a promising source of novel anticancer agents. We recently showed that protoflavones display activity in MDR cancer cell lines that overexpress the P-glycoprotein (P-gp) drug efflux pump. In this study, 52 protoflavones, including 22 new derivatives, were synthesized and tested against a panel of drug-sensitive parental cells and their MDR derivatives obtained by transfection with the human ABCB1 or ABCG2 genes, or by adaptation to chemotherapeutics. With the exception of protoapigenone, identified as a weak ABCG2 substrate, all protoflavones bypass resistance conferred by these two transporters. The majority of the compounds were found to exhibit mild to strong (up to 13-fold) selectivity against the MCF-7Dox and KB-V1 cell lines, but not to transfected MDR cells engineered to overexpress the MDR transporters. Our results suggest that protoflavones can overcome MDR cancer by evading P-gp-mediated efflux.
- Dankó, Balázs,Tóth, Szilárd,Martins, Ana,Vágv?lgyi, Máté,Kúsz, Norbert,Molnár, Joseph,Chang, Fang-Rong,Wu, Yang-Chang,Szakács, Gergely,Hunyadi, Attila
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p. 850 - 859
(2017/06/13)
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- COMPOSITION FOR TREATING CANCER CELLS AND SYNTHETIC METHOD FOR THE SAME
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A pharmaceutical composition having a cytotoxic effect to a cancer cell and a method for the same are provided. The pharmaceutical composition comprises a flavonoid compound having at least one of the following formulas: wherein B ring is a 4-oxo-cyclohex
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Page/Page column 3
(2009/04/24)
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- Composition for treating cancer cells and synthetic method for the same
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A pharmaceutical composition having a cytotoxic effect to a cancer cell and a method for the same are provided. The pharmaceutical composition comprises a flavonoid compound having at least one of the following formulas: and wherein B ring is a 4-oxo-cycl
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Page/Page column 6
(2008/12/04)
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