Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity
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 evaluat...
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MDPI AG,
2023-03-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_1bf026d25dac436d98c79f50adf8e463 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Sougata Santra |e author |
| 700 | 1 | 0 | |a Ainur D. Sharapov |e author |
| 700 | 1 | 0 | |a Ramil F. Fatykhov |e author |
| 700 | 1 | 0 | |a Anastasya P. Potapova |e author |
| 700 | 1 | 0 | |a Igor A. Khalymbadzha |e author |
| 700 | 1 | 0 | |a Maria I. Valieva |e author |
| 700 | 1 | 0 | |a Dmitry S. Kopchuk |e author |
| 700 | 1 | 0 | |a Grigory V. Zyryanov |e author |
| 700 | 1 | 0 | |a Alexander S. Bunev |e author |
| 700 | 1 | 0 | |a Vsevolod V. Melekhin |e author |
| 700 | 1 | 0 | |a Vasiliy S. Gaviko |e author |
| 700 | 1 | 0 | |a Andrey A. Zonov |e author |
| 245 | 0 | 0 | |a Xanthone-1,2,4-triazine and Acridone-1,2,4-triazine Conjugates: Synthesis and Anticancer Activity |
| 260 | |b MDPI AG, |c 2023-03-01T00:00:00Z. | ||
| 500 | |a 10.3390/ph16030403 | ||
| 500 | |a 1424-8247 | ||
| 520 | |a 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 (<b>7a</b>, <b>7e</b>, <b>9e</b>, <b>14a</b>, and <b>14b</b>) displayed good in vitro antiproliferative activities against these cancer cell lines. Compounds <b>7a</b> and <b>7e</b> 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 <b>7e</b> activates apoptotic mechanisms and inhibits proliferation in glioblastoma cells. | ||
| 546 | |a EN | ||
| 690 | |a xanthone | ||
| 690 | |a acridone | ||
| 690 | |a 1,2,4-triazine | ||
| 690 | |a colorectal cancer HCT116 | ||
| 690 | |a glioblastoma A-172 | ||
| 690 | |a breast ductal carcinoma Hs578T | ||
| 690 | |a Medicine | ||
| 690 | |a R | ||
| 690 | |a Pharmacy and materia medica | ||
| 690 | |a RS1-441 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Pharmaceuticals, Vol 16, Iss 3, p 403 (2023) | |
| 787 | 0 | |n https://www.mdpi.com/1424-8247/16/3/403 | |
| 787 | 0 | |n https://doaj.org/toc/1424-8247 | |
| 856 | 4 | 1 | |u https://doaj.org/article/1bf026d25dac436d98c79f50adf8e463 |z Connect to this object online. |