Research output: Contribution to journal › Article › peer-review
Research output: Contribution to journal › Article › peer-review
}
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