Remarkable Enhancement in Boron Uptake Within Glioblastoma Cells With Carboranyl-Indole Carboxamides
Access status:
Open Access
Type
ArticleAuthor/s
Narlawar, RajeshwarAustin, Christopher J. D.
Kahlert, Jan
Selleri, Silvia
Da Pozzo, Eleonora
Martini, Claudia
Werry, Eryn L.
Rendina, Louis M.
Kassiou, Michael
Abstract
Novel boron‐rich, carboranyl–indole carboxamide ligands were prepared and found to effectively target the 18 kDa translocator protein (TSPO), an upregulated mitochondrial membrane‐bound protein which has been observed in variety of tumor cell lines and its expression appears to be ...
See moreNovel boron‐rich, carboranyl–indole carboxamide ligands were prepared and found to effectively target the 18 kDa translocator protein (TSPO), an upregulated mitochondrial membrane‐bound protein which has been observed in variety of tumor cell lines and its expression appears to be proportional to the degree of tumorigenicity, emphasizing a key role in cancer cell proliferation. Both boronated compounds displayed remarkably high affinities for the TSPO. In addition, the in vitro uptake of these compounds into T98G human glioma cells was found to be 25‐ to 100‐fold greater than that of clinical boron neutron capture therapy (BNCT) agents.
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See moreNovel boron‐rich, carboranyl–indole carboxamide ligands were prepared and found to effectively target the 18 kDa translocator protein (TSPO), an upregulated mitochondrial membrane‐bound protein which has been observed in variety of tumor cell lines and its expression appears to be proportional to the degree of tumorigenicity, emphasizing a key role in cancer cell proliferation. Both boronated compounds displayed remarkably high affinities for the TSPO. In addition, the in vitro uptake of these compounds into T98G human glioma cells was found to be 25‐ to 100‐fold greater than that of clinical boron neutron capture therapy (BNCT) agents.
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Date
2018-10-17Publisher
Wiley‐VCH Verlag GmbH & Co. KGaA, WeinheimLicence
OtherFaculty/School
Faculty of Science, School of ChemistryCitation
Chem. Asian J. 2018, 13, 3321-3327Share