288401-01-4Relevant academic research and scientific papers
Synthesis and SAR Study of Anticancer Protoflavone Derivatives: Investigation of Cytotoxicity and Interaction with ABCB1 and ABCG2 Multidrug Efflux Transporters
Dankó, Balázs,Tóth, Szilárd,Martins, Ana,Vágv?lgyi, Máté,Kúsz, Norbert,Molnár, Joseph,Chang, Fang-Rong,Wu, Yang-Chang,Szakács, Gergely,Hunyadi, Attila
, p. 850 - 859 (2017/06/13)
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.
COMPOSITION FOR AMYLOID-ASSOCIATED DISEASE DIAGNOSIS
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Page/Page column 5; 34; 44; 52, (2010/11/28)
A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein,
Radioiodinated flavones for in vivo imaging of β-amyloid plaques in the brain
Ono, Masahiro,Yoshida, Naoko,Ishibashi, Kenichi,Haratake, Mamoru,Arano, Yasushi,Mori, Hiroshi,Nakayama, Morio
, p. 7253 - 7260 (2007/10/03)
In vivo imaging of β-amyloid (Aβ) peptide aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of AD treatment. The purpose of this study was to develop novel amyloid imaging a
