1. Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells
- Author
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Dmitry A. Gruzdev, Angelina A. Telegina, Galina L. Levit, Olga I. Solovieva, Tatiana Ya. Gusel’nikova, Ivan A. Razumov, Victor P. Krasnov, and Valery N. Charushin
- Subjects
folic acid ,amides ,carboranes ,cytotoxicity ,MTT assay ,tumour cells ,Biology (General) ,QH301-705.5 ,Chemistry ,QD1-999 - Abstract
The design of highly selective low-toxic, low-molecular weight agents for boron delivery to tumour cells is of decisive importance for the development of boron neutron capture therapy (BNCT), a modern efficient combined method for cancer treatment. In this work, we developed a simple method for the preparation of new closo- and nido-carborane-containing folic acid bis-amides containing 18–20 boron atoms per molecule. Folic acid derivatives containing nido-carborane residues were characterised by high water solubility, low cytotoxicity, and demonstrated a good ability to deliver boron to tumour cells in in vitro experiments (up to 7.0 µg B/106 cells in the case of U87 MG human glioblastoma cells). The results obtained demonstrate the high potential of folic acid–nido-carborane conjugates as boron delivery agents to tumour cells for application in BNCT.
- Published
- 2022
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