Research output: Contribution to journal › Article › peer-review
Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells. / Gruzdev, Dmitry A.; Telegina, Angelina A.; Levit, Galina L. et al.
In: International Journal of Molecular Sciences, Vol. 23, No. 22, 13726, 11.2022.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells
AU - Gruzdev, Dmitry A.
AU - Telegina, Angelina A.
AU - Levit, Galina L.
AU - Solovieva, Olga I.
AU - Gusel’nikova, Tatiana Ya
AU - Razumov, Ivan A.
AU - Krasnov, Victor P.
AU - Charushin, Valery N.
N1 - Funding Information: This research was funded by the Russian Science Foundation, grant number 21-73-10073. Publisher Copyright: © 2022 by the authors.
PY - 2022/11
Y1 - 2022/11
N2 - 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.
AB - 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.
KW - amides
KW - BNCT
KW - boron accumulation
KW - carboranes
KW - cytotoxicity
KW - folic acid
KW - MTT assay
KW - tumour cells
KW - Humans
KW - Glioblastoma
KW - Amides
KW - Thinness
KW - Boron/pharmacology
KW - Folic Acid/pharmacology
UR - http://www.scopus.com/inward/record.url?scp=85142607924&partnerID=8YFLogxK
UR - https://www.mendeley.com/catalogue/bfcde324-57cc-3975-a35e-e1bff34a4861/
U2 - 10.3390/ijms232213726
DO - 10.3390/ijms232213726
M3 - Article
C2 - 36430206
AN - SCOPUS:85142607924
VL - 23
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
SN - 1661-6596
IS - 22
M1 - 13726
ER -
ID: 40002784