European Journal of Medicinal Chemistry p. 884 - 889 (2017)
Update date:2022-08-15
Topics:
Santos, Mariana B.
Pinhanelli, Vitor C.
Garcia, Mayara A.R.
Silva, Gabriel
Baek, Seung J.
Fran?a, Suzelei C.
Fachin, Ana L.
Marins, Mozart
Regasini, Luis O.
In the present study, a series of 2′- and 4′-aminochalcones were synthesized and their antiproliferative activity against a canine malignant histiocytic cell line (DH82) was evaluated. Particularly aminochalcones with a hydrophobic substituent on ring B proved to be potent antiproliferative agents. Among these compounds, aminochalcones 3, 4 and 11 inhibited the growth of DH82 cells, with IC50 values of 34.4, 31.4 and 38.2 μM, respectively, and were three times more potent than etoposide (IC50 = 95.5 μM). The selected chalcones induced death through apoptosis rather than necrosis in DH82 and non-tumorigenic Madin-Darby canine kidney cells (MDCK). Further experiments suggested that the aminochalcones interfere with the regulation of oncogenes/tumor suppressor genes. Aminochalcone 11 inhibited transcription of the TOPOIIα and TP53 genes and aminochalcone 4 down-regulated Sp1 protein expression in a concentration-dependent manner.
View MoreShanghai Haoyuan Chemexpress Co., Ltd.
Contact:86-21-51870955;58998985;58999585
Address:Room 601, No. 2 BLD, NO. 720, Cailun Road, Zhangjiang, Shanghai, China
Ningbo Hi-tech Zone Nice-Synth Chemical Industry Ltd.
Contact:+86-(574)-81110986
Address:No. 1210, Building 3, Wante Business Centre, Hi-tech Zone, Ningbo
Xiamen XM-Innovation Chemical Co., Ltd
Contact:+86-592-3216205
Address:Unit Q, 11/F, No.1 Office Building, Wuyuan Bay Business Center, Huli District, Xiamen City, Fujian Province, P.R.C
ChangZhou XiaQing Chemical Co., Ltd.
Contact:+86-519-88721665
Address:3# Hengluo Road, Henglin Town, Changzhou City, Jiangsu Province,China
Jiangsu Jiuri Chemical Co.,Ltd.
Contact:+86-519-82118868
Address:Tianwang Town, Jurong City, Jiangsu Province, China
Doi:10.3184/174751916X14639973714726
(2016)Doi:10.1016/j.jorganchem.2005.01.018
(2005)Doi:10.1021/jacs.1c06408
(2021)Doi:10.1007/s11094-015-1285-x
(2015)Doi:10.1002/chem.201101839
(2011)Doi:10.1002/1521-3765(20021115)8:22<5204::AID-CHEM5204>3.0.CO;2-C
(2002)