Bioorganic and Medicinal Chemistry Letters p. 2957 - 2960 (2018)
Update date:2022-08-03
Topics:
Huang, Yaping
Sun, Geng
Wang, Pengfei
Shi, Rui
Zhang, Yanchun
Wen, Xiaoan
Sun, Hongbin
Chen, Caiping
In this study, Complex I inhibitor R419 was firstly revealed to have significant anticancer activity against HepG2 cells (IC50 = 5.2 ± 0.9 μM). Based on this finding, a series of R419 derivatives were synthesized and biologically evaluated. As results, 9 derivatives were found to have obvious anticancer activity. Among them, H20 exhibited the most potent activity (IC50 = 2.8 ± 0.4 μM). Mechanism study revealed that H20 caused severe depletion of cellular ATP, dose-dependently activated AMPK, decreased Bcl-2/Bax ratio and induced necrotic cell death. Most importantly, H20 displayed definite inhibitory activity against Complex I.
View Morewebsite:http://www.apeptides.com/en/
Contact:+86-21-60871011
Address:No. 80 Chuanshan Shuyuan Steet,Pudong,Shanghai
SuZhou Hua-Emy Chemical Import and Export Co., LTD.
Contact:+86-512-88804994; +86-512-88804550;
Address:710, Building B, International Trade Center, 12 Huanghelu, Changshu, Jiangsu,China
Shandong Jiulong Hisince Pharmaceutical Co.,Ltd.
Contact:+86-15853188990
Address:Huadian Pioneer Park, Huadian Township, Qihe County, Dezhou City, Shandong, P.R.China
shijiazhuang shuanglian chemical industry co.,ltd
Contact:0311-82190302
Address:Luquan Intersection , Shijiazhuang--Taiyuan Expressway,Shijiazhuang City
Contact:+86-532-80762375
Address:No. 6, Hongkong Middle Road, Qingdao, China
Doi:10.1016/j.tet.2013.05.064
(2013)Doi:10.1007/s10593-005-0179-3
(2005)Doi:10.1016/S0040-4039(01)91051-2
(1984)Doi:10.1016/j.tet.2006.12.088
(2007)Doi:10.1016/j.tetlet.2006.12.109
(2007)Doi:10.1016/j.apcata.2014.08.009
(2014)