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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 journalArticlepeer-review

Harvard

Gruzdev, DA, Telegina, AA, Levit, GL, Solovieva, OI, Gusel’nikova, TY, Razumov, IA, Krasnov, VP & Charushin, VN 2022, 'Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells', International Journal of Molecular Sciences, vol. 23, no. 22, 13726. https://doi.org/10.3390/ijms232213726

APA

Gruzdev, D. A., Telegina, A. A., Levit, G. L., Solovieva, O. I., Gusel’nikova, T. Y., Razumov, I. A., Krasnov, V. P., & Charushin, V. N. (2022). Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells. International Journal of Molecular Sciences, 23(22), [13726]. https://doi.org/10.3390/ijms232213726

Vancouver

Gruzdev DA, Telegina AA, Levit GL, Solovieva OI, Gusel’nikova TY, Razumov IA et al. Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells. International Journal of Molecular Sciences. 2022 Nov;23(22):13726. doi: 10.3390/ijms232213726

Author

Gruzdev, Dmitry A. ; Telegina, Angelina A. ; Levit, Galina L. et al. / Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells. In: International Journal of Molecular Sciences. 2022 ; Vol. 23, No. 22.

BibTeX

@article{549f14a25a6649a79f9e817119fb39b9,
title = "Carborane-Containing Folic Acid bis-Amides: Synthesis and In Vitro Evaluation of Novel Promising Agents for Boron Delivery to Tumour Cells",
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.",
keywords = "amides, BNCT, boron accumulation, carboranes, cytotoxicity, folic acid, MTT assay, tumour cells, Humans, Glioblastoma, Amides, Thinness, Boron/pharmacology, Folic Acid/pharmacology",
author = "Gruzdev, {Dmitry A.} and Telegina, {Angelina A.} and Levit, {Galina L.} and Solovieva, {Olga I.} and Gusel{\textquoteright}nikova, {Tatiana Ya} and Razumov, {Ivan A.} and Krasnov, {Victor P.} and Charushin, {Valery N.}",
note = "Funding Information: This research was funded by the Russian Science Foundation, grant number 21-73-10073. Publisher Copyright: {\textcopyright} 2022 by the authors.",
year = "2022",
month = nov,
doi = "10.3390/ijms232213726",
language = "English",
volume = "23",
journal = "International Journal of Molecular Sciences",
issn = "1661-6596",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "22",

}

RIS

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