European Journal of Medicinal Chemistry p. 1919 - 1930 (2018)
Update date:2022-08-03
Topics:
Ramisetti, Srinivasa Rao
Pandey, Manoj K.
Lee, Sang Y.
Karelia, Deepkamal
Narayan, Satya
Amin, Shantu
Sharma, Arun K.
A series of novel thio- and seleno-barbituric acid derivatives were synthesized by varying the substituents at N1 and N3 (ethyl, methyl, allyl, and phenyl), and C5 tethered with dienyl and trienyl moieties attached to substituents such as phenyl, 2-furanyl, 2-thiophenyl, 1-naphthyl, and 3-pyridyl. The cytotoxic potential of these derivatives was evaluated by using MTT assay against melanoma cell lines expressing either wild-type (CHL-1) or mutant (UACC 903) BRAF gene. Among all, 2b and 8b were identified as the most potent compounds. Both 2b and 8b inhibited viability of various melanoma cells and induced cell death as evidenced by Live and Dead assay. Western blot analysis showed that they induce PARP cleavage and inhibit anti-apoptotic Bcl-2, Bcl-xL and Survivin in a dose-dependent manner within 24 h of the treatment. Novel thiobarbituric acid analogs also inhibited viability of various other solid tumor cell lines, such as pancreatic, breast, and colon. Overall, 2b, 2d, and 8b emerged as the most effective compounds and make good leads for the development of future therapeutic agents.
View MoreZhejiang Chemicals Import & Export Corporation
Contact:86-571-87043088
Address:No.37,Qingchun Road,Hangzhou,China
Contact:025-86793338
Address:nanjing jiangsu
Henan Tianfu Chemical Co., Ltd.
website:http://www.tianfuchem.com
Contact:86-371-55170693/55170694
Address:Zhengzhou International Trade New Territory,Jinshui District,Zhengzhou ,China
Hangzhou Zyter Biological & Chemical Technology Co., Ltd.
website:http://www.zyterpharm.com
Contact:+86-18858184290
Address:West Wenyi Road, Cangqian, Yuhang
Contact:021-36356756
Address:Room601,Building No.14,280 Yangcheng Road,Shanghai
Doi:10.1080/15421406.2014.939598
(2015)Doi:10.1021/jo961861m
(1998)Doi:10.1016/j.bmcl.2018.04.057
(2018)Doi:10.3987/COM-97-S24
(1997)Doi:10.1021/acs.jnatprod.6b00581
(2016)Doi:10.1002/(SICI)1099-0690(199803)1998:3<493::AID-EJOC493>3.0.CO;2-N
(1998)