Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity
Электронный научный архив УРФУ
Информация об архиве | Просмотр оригинала| Поле | Значение | |
| Заглавие |
Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity
|
|
| Автор |
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. |
|
| Тематика |
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 |
|
| Описание |
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.
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). |
|
| Дата |
2024-04-05T16:19:00Z
2024-04-05T16:19:00Z 2023 |
|
| Тип |
Article
Journal article (info:eu-repo/semantics/article) |info:eu-repo/semantics/publishedVersion |
|
| Идентификатор |
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 1424-8247 Final All Open Access, Gold, Green https://www.scopus.com/inward/record.uri?eid=2-s2.0-85151615999&doi=10.3390%2fph16030403&partnerID=40&md5=6262f6d39813b5317f35563fa6434c5f https://www.mdpi.com/1424-8247/16/3/403/pdf?version=1678237560 http://elar.urfu.ru/handle/10995/130367 10.3390/ph16030403 85151615999 000956929400001 |
|
| Язык |
en
|
|
| Права |
Open access (info:eu-repo/semantics/openAccess)
cc-by https://creativecommons.org/licenses/by/4.0/ |
|
| Формат |
application/pdf
|
|
| Издатель |
MDPI
|
|
| Источник |
Pharmaceuticals
Pharmaceuticals |
|