1069051-42-8Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents
Cheng, Gaoliang,Wang, Zhi,Yang, Jinyu,Bao, Yu,Xu, Qihao,Zhao, Linxiang,Liu, Dan
, p. 410 - 417 (2019/01/03)
HDAC inhibitors and BRD4 inhibitors were considered to be potent anti-cancer agents. Recent studies have demonstrated that HDAC and BRD4 participate in the regulation of some signal paths like PI3K-AKT. In this work, a series of indole derivatives that co
Intermolecular dearomative C2-arylation of N-Ac indoles activated by FeCl3
Nandi, Raj Kumar,Ratsch, Friederike,Beaud, Rodolphe,Guillot, Régis,Kouklovsky, Cyrille,Vincent, Guillaume
, p. 5328 - 5331 (2016/04/26)
We report the FeCl3-mediated direct addition of electron-rich arenes to the C2-position of electrophilic N-Ac indoles under mild conditions (room temperature, air). No functional group is required on the arene nucleophile: one of its C-H bonds is added to the C2=C3 double bond of the indole nucleus in a Friedel-Crafts-type reaction. This dearomatisation process delivered a broad range of C2-arylated indolines.
Design, synthesis, and biological evaluation of 3-(1-aryl-1 h -indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase a2α inhibitors
Tomoo, Toshiyuki,Nakatsuka, Takashi,Katayama, Toyoko,Hayashi, Yasuhiro,Fujieda, Yusuke,Terakawa, Maki,Nagahira, Kazuhiro
, p. 7244 - 7262 (2015/01/30)
This article describes the design, synthesis, and biological evaluation of new indole-based cytosolic phospholipase A2α (cPLA2α, a group IVA phospholipase A2) inhibitors. A screening-hit compound from our library, (E)-3-{4-[(4-chlorophenyl)thio]-3-nitrophenyl}acrylic acid (5), was used to design a class of 3-(1-aryl-1H-indol-5-yl)propanoic acids as new small molecule inhibitors. The resultant structure-activity relationships studied using the isolated enzyme and by cell-based assays revealed that the 1-(p-O-substituted)phenyl, 3-phenylethyl, and 5-propanoic acid groups on the indole core are essential for good inhibitory activity against cPLA2α. Optimization of the p-substituents on the N1 phenyl group led to the discovery of 56n (ASB14780), which was shown to be a potent inhibitor of cPLA2α via enzyme assay, cell-based assay, and guinea pig and human whole-blood assays. It displayed oral efficacy toward mice tetradecanoyl phorbol acetate-induced ear edema and guinea pig ovalbumin-induced asthma models.
INDOLE DERIVATIVE HAVING CPLA2 INHIBITORY ACTIVITY, USE OF THE SAME AND METHOD FOR PRODUCING THE SAME
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Page/Page column 23, (2010/01/29)
A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
