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

Santra, S.; Sharapov, A. D.; Fatykhov, R. F.; Potapova, A. P.; Khalymbadzha, I. A.; Valieva, M. I.; Kopchuk, D. S.; Zyryanov, G. V.; Bunev, A. S.; Melekhin, V. V.; Gaviko, V. S.; Zonov, A. A.

doi:10.3390/ph16030403

Please use this identifier to cite or link to this item: http://elar.urfu.ru/handle/10995/130367

Title:	Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity
Authors:	Santra, S. Sharapov, A. D. Fatykhov, R. F. Potapova, A. P. Khalymbadzha, I. A. Valieva, M. I. Kopchuk, D. S. Zyryanov, G. V. Bunev, A. S. Melekhin, V. V. Gaviko, V. S. Zonov, A. A.
Issue Date:	2023
Publisher:	MDPI
Citation:	Santra, S, Sharapov, AD, Fatykhov, RF, Potapova, AP, Khalymbadzha, IA, Valieva, MI, Kopchuk, DS, Zyryanov, GV, Bunev, AS, Melekhin, VV, Gaviko, VS & Zonov, AA 2023, 'Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity', Pharmaceuticals, Том. 16, № 3, 403. https://doi.org/10.3390/ph16030403 Santra, S., Sharapov, A. D., Fatykhov, R. F., Potapova, A. P., Khalymbadzha, I. A., Valieva, M. I., Kopchuk, D. S., Zyryanov, G. V., Bunev, A. S., Melekhin, V. V., Gaviko, V. S., & Zonov, A. A. (2023). Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity. Pharmaceuticals, 16(3), [403]. https://doi.org/10.3390/ph16030403
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. © 2023 by the authors.
Keywords:	1,2,4-TRIAZINE ACRIDONE BREAST DUCTAL CARCINOMA HS578T COLORECTAL CANCER HCT116 GLIOBLASTOMA A-172 XANTHONE 1 HYDROXY 3 METHOXY 10 METHYL 2 (3 PHENYL 6 (4 TOLYL) 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) ACRIDIN 9 (10H) ONE 1 HYDROXY 3 METHOXY 10 METHYL 2 (5 PHENYL [2,2' BIPYRIDIN] 6 YL)ACRIDIN 9 (10H)ONE 1 HYDROXY 3 METHOXY 10 METHYL 2 (6 PHENYL 3 (PYRIDIN 2 YL) 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) ACRIDIN 9 (10H) ONE 1 HYDROXY 3 METHOXY 10 METHYLACRIDIN 9 (10H) ONE 1 HYDROXY 3 METHOXY 2 [6 (4 METHOXYPHENYL) 3 (PYRIDIN 2 YL) 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL] 10 METHYLACRIDIN 9 (10H) ONE 1,3 DIHYDROXY 4 [3 (METHYLTHIO) 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL] 9H XANTHEN 9 ONE 2 (3,6 DIPHENYL 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) 1 HYDROXY 3 METHOXY 10 METHYLACRIDIN 9 (10H) ONE 2 (3,6 DIPHENYLPYRIDIN 2 YL) 1 HYDROXY 3 METHOXY 10 METHYLACRIDIN 9 (10H)ONE 2 [3,6 BIS(4 METHOXYPHENYL) 1,2,4 TRIAZIN 5 YL] 1 HYDROXY 3 METHOXY 10 METHYLACRIDIN 9 (10H)ONE 2 [3,6 BIS(4 METHOXYPHENYL) 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL] 1 HYDROXY 3 METHOXY 10 METHYLACRIDIN 9 (10H) ONE 4 (3,6 DIPHENYL 1,2,4 TRIAZIN 5 YL) 1,3,6 TRIMETHOXY 9H XANTHEN 9 ONE 4 (3,6 DIPHENYL 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) 1,3 DIHYDROXY 9H XANTHEN 9 ONE 4 (3,6 DIPHENYL 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) 1,3 DIMETHOXY 9H XANTHEN 9 ONE 4 (3,6 DIPHENYL 2,5 DIHYDRO 1,2,4 TRIAZIN 5 YL) 1,3,6 TRIMETHOXY 9H XANTHEN 9 ONE ACRIDONE 1,2,4 TRIAZINE ANTINEOPLASTIC AGENT CISPLATIN CYTOTOXIC AGENT ETOPOSIDE UNCLASSIFIED DRUG XANTHONE 1,2,4 TRIAZINE A-172 CELL LINE ANTINEOPLASTIC ACTIVITY APOPTOSIS ARTICLE CARBON NUCLEAR MAGNETIC RESONANCE CELL VIABILITY CONTROLLED STUDY DRUG CYTOTOXICITY DRUG DETERMINATION DRUG EFFECT DRUG STRUCTURE DRUG SYNTHESIS EMBRYO HCT 116 CELL LINE HEK293 CELL LINE HS 578T CELL LINE HUMAN HUMAN CELL IC50 PROTON NUCLEAR MAGNETIC RESONANCE SUBSTITUTION REACTION
URI:	http://elar.urfu.ru/handle/10995/130367
Access:	info:eu-repo/semantics/openAccess cc-by
License text:	https://creativecommons.org/licenses/by/4.0/
SCOPUS ID:	85151615999
WOS ID:	000956929400001
PURE ID:	37086149
ISSN:	1424-8247
DOI:	10.3390/ph16030403
metadata.dc.description.sponsorship:	Ministry of Education and Science of the Russian Federation, Minobrnauka: FEUZ-2023-0021, H687.42B.325/23 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).
Appears in Collections:	Научные публикации ученых УрФУ, проиндексированные в SCOPUS и WoS CC

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