Результаты исследований: Вклад в журнал › Статья › Рецензирование
Результаты исследований: Вклад в журнал › Статья › Рецензирование
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TY - JOUR
T1 - 5-Alkylamino-7-aminoazolo[1,5-a]pyrimidine-6-carbonitriles: synthetic strategies and anticancer activity in vitro
AU - Urakov, G. v.
AU - Savateev, K. v.
AU - Melekhin, V. v.
AU - Kotovskaya, S. k.
AU - Rusinov, V. l.
N1 - The study was supported by the Ministry of Science and Higher Education of the Russian Federation (state contract No. FEUZ-2023-0021 (H687/42B.325/23)).
PY - 2023/12/1
Y1 - 2023/12/1
N2 - The design of novel antagonists for adenosine A2a receptor (A2a AR) is a promising strategy for the development of new-generation anticancer agents. 5-Alkylamino-7-aminoazolo[1,5-a]pyrimidin-6-carbonitriles proposed in this work are close structural analogs of known nanomolar A2a AR antagonists. An efficient synthetic strategy towards the functional derivatives of the target heterocycles is cyclocondensation of aminoazoles with 2-[(alkylamino)(methylsulfanyl)methylene]malononitriles on heating in DMF in the presence of ButOK. The obtained azolopyrimidine-6-carbonitriles do not show statistically significant cytotoxic effect on human embryonic kidney cells, while 2-methyl- and 2-(furan-2-yl)azolopyrimidines inhibit the viability of lung carcinoma and hepatocellular carcinoma cells with IC50 values in the low micromolar range.
AB - The design of novel antagonists for adenosine A2a receptor (A2a AR) is a promising strategy for the development of new-generation anticancer agents. 5-Alkylamino-7-aminoazolo[1,5-a]pyrimidin-6-carbonitriles proposed in this work are close structural analogs of known nanomolar A2a AR antagonists. An efficient synthetic strategy towards the functional derivatives of the target heterocycles is cyclocondensation of aminoazoles with 2-[(alkylamino)(methylsulfanyl)methylene]malononitriles on heating in DMF in the presence of ButOK. The obtained azolopyrimidine-6-carbonitriles do not show statistically significant cytotoxic effect on human embryonic kidney cells, while 2-methyl- and 2-(furan-2-yl)azolopyrimidines inhibit the viability of lung carcinoma and hepatocellular carcinoma cells with IC50 values in the low micromolar range.
UR - http://www.scopus.com/inward/record.url?partnerID=8YFLogxK&scp=85183614877
UR - https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=tsmetrics&SrcApp=tsm_test&DestApp=WOS_CPL&DestLinkType=FullRecord&KeyUT=001154671000012
U2 - 10.1007/s11172-023-4114-5
DO - 10.1007/s11172-023-4114-5
M3 - Article
VL - 72
SP - 3022
EP - 3031
JO - Russian Chemical Bulletin
JF - Russian Chemical Bulletin
SN - 1066-5285
IS - 12
ER -
ID: 52301476