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Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity. / Santra, Sougata; Sharapov, Ainur D.; Fatykhov, Ramil F. et al.
In: Pharmaceuticals, Vol. 16, No. 3, 403, 2023.

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@article{5edf3c28a7024eda97c9ad021e8a56d8,
title = "Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity",
abstract = "A total of 21 novel xanthone and acridone derivatives were synthesized using the reactions of 1,2,4-triazine derivatives with 1-hydroxy-3-methoxy-10-methylacridone, 1,3-dimethoxy-, and 1,3-dihydroxanthone, followed by optional dihydrotiazine ring aromatization. The synthesized compounds were evaluated for their anticancer activity against colorectal cancer HCT116, glioblastoma A-172, breast cancer Hs578T, and human embryonic kidney HEK-293 tumor cell lines. Five compounds (7a, 7e, 9e, 14a, and 14b) displayed good in vitro antiproliferative activities against these cancer cell lines. Compounds 7a and 7e demonstrated low toxicity for normal human embryonic kidney (HEK-293) cells, which determines the possibility of further development of these compounds as anticancer agents. Annexin V assay demonstrated that compound 7e activates apoptotic mechanisms and inhibits proliferation in glioblastoma cells.",
author = "Sougata Santra and Sharapov, {Ainur D.} and Fatykhov, {Ramil F.} and Potapova, {Anastasya P.} and Khalymbadzha, {Igor A.} and Valieva, {Maria I.} and Kopchuk, {Dmitry S.} and Zyryanov, {Grigory V.} and Bunev, {Alexander S.} and Melekhin, {Vsevolod V.} and Gaviko, {Vasiliy S.} and Zonov, {Andrey A.}",
note = "This research was funded by the Ministry of Science and Higher Education of the Russian Federation, State Contract no FEUZ-2023-0021 (H687.42B.325/23).",
year = "2023",
doi = "10.3390/ph16030403",
language = "English",
volume = "16",
journal = "Pharmaceuticals",
issn = "1424-8247",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "3",

}

RIS

TY - JOUR

T1 - Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity

AU - Santra, Sougata

AU - Sharapov, Ainur D.

AU - Fatykhov, Ramil F.

AU - Potapova, Anastasya P.

AU - Khalymbadzha, Igor A.

AU - Valieva, Maria I.

AU - Kopchuk, Dmitry S.

AU - Zyryanov, Grigory V.

AU - Bunev, Alexander S.

AU - Melekhin, Vsevolod V.

AU - Gaviko, Vasiliy S.

AU - Zonov, Andrey A.

N1 - This research was funded by the Ministry of Science and Higher Education of the Russian Federation, State Contract no FEUZ-2023-0021 (H687.42B.325/23).

PY - 2023

Y1 - 2023

N2 - A total of 21 novel xanthone and acridone derivatives were synthesized using the reactions of 1,2,4-triazine derivatives with 1-hydroxy-3-methoxy-10-methylacridone, 1,3-dimethoxy-, and 1,3-dihydroxanthone, followed by optional dihydrotiazine ring aromatization. The synthesized compounds were evaluated for their anticancer activity against colorectal cancer HCT116, glioblastoma A-172, breast cancer Hs578T, and human embryonic kidney HEK-293 tumor cell lines. Five compounds (7a, 7e, 9e, 14a, and 14b) displayed good in vitro antiproliferative activities against these cancer cell lines. Compounds 7a and 7e demonstrated low toxicity for normal human embryonic kidney (HEK-293) cells, which determines the possibility of further development of these compounds as anticancer agents. Annexin V assay demonstrated that compound 7e activates apoptotic mechanisms and inhibits proliferation in glioblastoma cells.

AB - A total of 21 novel xanthone and acridone derivatives were synthesized using the reactions of 1,2,4-triazine derivatives with 1-hydroxy-3-methoxy-10-methylacridone, 1,3-dimethoxy-, and 1,3-dihydroxanthone, followed by optional dihydrotiazine ring aromatization. The synthesized compounds were evaluated for their anticancer activity against colorectal cancer HCT116, glioblastoma A-172, breast cancer Hs578T, and human embryonic kidney HEK-293 tumor cell lines. Five compounds (7a, 7e, 9e, 14a, and 14b) displayed good in vitro antiproliferative activities against these cancer cell lines. Compounds 7a and 7e demonstrated low toxicity for normal human embryonic kidney (HEK-293) cells, which determines the possibility of further development of these compounds as anticancer agents. Annexin V assay demonstrated that compound 7e activates apoptotic mechanisms and inhibits proliferation in glioblastoma cells.

UR - https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=tsmetrics&SrcApp=tsm_test&DestApp=WOS_CPL&DestLinkType=FullRecord&KeyUT=000956929400001

UR - http://www.scopus.com/inward/record.url?partnerID=8YFLogxK&scp=85151615999

U2 - 10.3390/ph16030403

DO - 10.3390/ph16030403

M3 - Article

VL - 16

JO - Pharmaceuticals

JF - Pharmaceuticals

SN - 1424-8247

IS - 3

M1 - 403

ER -

ID: 37086149