- Design, synthesis and biological evaluations of diverse Michael acceptor-based phenazine hybrid molecules as TrxR1 inhibitors
-
A series of novel phenazine derivatives (1~27) containing the Michael acceptor scaffolds were designed and synthesized in this study. Some compounds exhibited selective cytotoxicity against Bel-7402 cancer cell line in vitro, in which compound 26 were found to have the best antiproliferative activity. Meanwhile, compound 26 showed no obvious cell toxicity against human normal liver epithelial L02 cells, which means this compound possessed a better safety potential. In the following research, compound 26 was verified to inhibit TrxR1 enzyme activity, ultimately resulting in cellular molecular mechanism events of apoptosis including growth of intracellular ROS level, depletion of reduced Trx1, liberation of ASK1 and up-regulation of p38, respectively. Together, all these evidences implicated that compound 26 acted as the TrxR1 inhibitor against Bel-7402 cells, and could activate apoptosis through the ROS-Trx-ASK1-p38 pathway.
- Zhong, Yucheng,Liu, Jing,Cheng, Xiangyu,Zhang, Hao,Zhang, Chunhua,Xia, Zhuolu,Wu, Zhongxi,Zhang, Lu,Zheng, Yuting,Gao, Zhanyu,Jiang, Zhidong,Wang, Zhixiang,Huang, Dechun,Lu, Yuanyuan,Jiang, Feng
-
-
- Synthesis and anticancer activity of some novel 2-phenazinamine derivatives
-
In this study, we report the synthesis and spectral characterization of a novel series of 2-phenazinamine derivatives. In vitro evaluation for their anticancer activity toward cultured K562 (human chronic myelogenous leukemia), HepG2 (human hepatocellular
- Gao, Xiaochun,Lu, Yuanyuan,Fang, Lei,Fang, Xubin,Xing, Yingying,Gou, Shaohua,Xi, Tao
-
-
- ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION
-
Compounds, methods and pharmaceutical compositions for treating viral : infections, by administering certain novel compounds in therapeutically effective "'" amounts are disclosed. Methods for preparing the compounds and method’s using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
- -
-
Page/Page column 40
(2008/06/13)
-
- Novel benzimidazole-based MCH R1 antagonists
-
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
- Carpenter, Andrew J.,Al-Barazanji, Kamal A.,Barvian, Kevin K.,Bishop, Michael J.,Britt, Christy S.,Cooper, Joel P.,Goetz, Aaron S.,Grizzle, Mary K.,Hertzog, Donald L.,Ignar, Diane M.,Morgan, Ronda O.,Peckham, Gregory E.,Speake, Jason D.,Swain, Will R.
-
p. 4994 - 5000
(2007/10/03)
-
- INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 AND TYPE 2
-
There is provided a compound having Formula (I): wherein one of R1 and R2 is a group of the Formula (a), wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group (Formula (a)) wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.
- -
-
Page/Page column 122; 123
(2010/02/06)
-
- Antibacterial water-soluble cutting fluids resistant to yeast-like fungi
-
A bactericide is added to conventional water-soluble cutting fluids to suppress deterioration by micro-organisms. Such fluids are however accompanied by the drawbacks that the bactericide has a narrow antibacterial spectrum and moreover its effects last a short time. It is the object of the present invention to offers water--soluble cutting fluids which remain resistant to a wide variety of microorganisms for a long time. The present invention therefore offers water-soluble cutting fluids to which has been added a specific amine selected from amines known to date.
- -
-
-