1069051-39-3

Upstream product

• 10075-50-0 5-bromo-1H-indole 
• 103-80-0 phenylacetyl chloride 
• 30516-21-3 1-(1H-benzo[d][1,2,3]triazol-1-yl)-2-phenylethan-1-one 
• 127876-36-2 2-(benzotriazol-1-yl)acetophenone 

Downstream Products

• 1069051-42-8 5-bromo-3-(2-phenylethyl)-1H-indole 
• 1069047-04-6 methyl (2E)-3-[3-(2-phenylethyl)-1H-indol-5-yl]-2-propenoate 
• 1069048-07-2 ethyl (2E)-3-[3-(2-phenylethyl)-1H-indol-5-yl]-2-propenoate 
• 1069047-06-8 methyl 3-[3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069048-09-4 ethyl 3-[3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069047-81-9 methyl 3-{1-[4-(benzyloxy)phenyl]-3-(2-phenylethyl)-1H-indol-5-yl}propanoate 
• 1069047-87-5 methyl 3-[1-(4-hydroxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069043-75-9 ethyl 3-{1-[3-(benzyloxy)phenyl]-3-(2-phenylethyl)-1H-indol-5-yl}propanoate 
• 1069043-79-3 ethyl 3-[1-(3-hydroxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1330658-89-3 ethyl 3-{1-[2-(benzyloxy)phenyl]-3-(2-phenylethyl)-1H-indol-5-yl}propanoate 
• 1069043-67-9 ethyl 3-[1-(2-hydroxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069042-93-8 methyl 3-[1-(4-methoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069043-35-1 methyl 3-[1-(4-ethoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 1069043-37-3 methyl 3-[3-(2-phenylethyl)-1-(4-n-propoxyphenyl)-1H-indol-5-yl]propanoate 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents

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

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

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.

A novel microwave-irradiated solvent-free 3-acylation of indoles on alumina

A simple and efficient 3-acylation of indoles under microwave-heated and solvent-free conditions is developed. This general procedure uses neutral Al2O3 as a new, green and reusable catalyst giving good to high yields within short reaction times. Utilizing such an environmentally- benign methodology, a variety of indoles bearing electron-releasing or electron-withdrawing groups were conveniently acylated.

INDOLE DERIVATIVE HAVING CPLA2 INHIBITORY ACTIVITY, USE OF THE SAME AND METHOD FOR PRODUCING THE SAME

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.