38470-64-3

Upstream product

• 703-80-0 3-acetylindole 
• 100-52-7 benzaldehyde 
• 120-72-9 indole 
• 102-92-1 Cinnamoyl chloride 
• 100-51-6 benzyl alcohol 

Downstream Products

• 15849-57-7 (E)-1-(1-methyl-1H-indol-3-yl)-3-phenylprop-2-en-1-one 
• 140472-59-9 5,5-dimethyl-2-(1'-methylindol-3'-yl)-4-phenyl-1-pyrroline 1-oxide 
• 140472-55-5 4-methyl-1-(1'-methylindol-3'-yl)-4-nitro-3-phenylpentan-1-one 
• 1410102-97-4 dimethyl 2-(3-(1H-indol-3-yl)-3-oxo-1-phenylpropyl)malonate 
• 1221963-05-8 2-[3-(1H-indol-3-yl)-3-oxo-1-phenylpropyl]malonic acid 
• 27664-19-3 3-(1,5-diphenyl-4,5-dihydro-1H-pyrazol-3-yl)-indole 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel indole-pyrazoline hybrid derivatives as potential topoisomerase 1 inhibitors

A series of novel indole-pyrazoline hybrid derivatives were designed, synthesized, and evaluated for topoisomerase 1 (Top1) inhibitory activity. Top1-mediated relaxation assays showed that our synthesized compounds had variable Top1 inhibitory activity. A

Identification of Indole-Based Chalcones: Discovery of a Potent, Selective, and Reversible Class of MAO-B Inhibitors

A series of 11 indole-based chalcones (IC1–11) with various electron donating and withdrawing groups at the para position of the phenyl ring B were synthesized. All the compounds were tested for their human monoamine oxidase (hMAO)-A and hMAO-B inhibitory

2-(3-oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: Development and prodrug concept

The protein kinase C-related kinase 2 (PRK2)-interacting fragment (PIF) pocket of phosphoinositide-dependent kinase-1 (PDK1) was proposed as a novel target site for allosteric modulators. In the present work, we describe the design, synthesis, and structure-activity relationship of a series of 2-(3-oxo-1,3-diphenylpropyl)malonic acids as potent allosteric activators binding to the PIF pocket. Some congeners displayed AC50 values for PDK1 activation in the submicromolar range. The potency of the best compounds to stabilize PDK1 in a thermal stability shift assay was in the same order of magnitude as that of the PIF pocket binding peptide PIFtide, suggesting comparable binding affinities to the PIF pocket. The crystal structure of PDK1 in complex with compound 4h revealed that additional ionic interactions are mainly responsible for the increased potency compared to the monocarboxylate analogues. Notably, several compounds displayed high selectivity for PDK1. Employing a prodrug strategy, we were able to corroborate the novel mechanism of action in cells.

Easy α-alkylation of ketones with alcohols through a hydrogen autotransfer process catalyzed by RuCl2(DMSO)4

The electrophilic α-alkylation of ketones with alcohols is accomplished by a hydrogen autotransfer process catalyzed by RuCl2(DMSO)4. The reaction can produce either simple alkylated ketones or α,β-unsaturated ketones just by choosing the appropriate starting ketones (methyl ketones or bicyclic methylenic ketones, respectively), as well as quinolines (by using 2-aminobenzyl alcohol derivatives) or the corresponding alcohol derivatives by the addition of an extra equivalent of the initial alcohol. In the last case, after the above alkylation process reduction of the carbonyl compound takes place. A mechanistic study seems to indicate that the process goes through the oxidation of the alcohols with ruthenium (after a previous deprotonation) to yield the corresponding aldehyde and a ruthenium hydride intermediate. In turn, the aldehyde suffers a classical aldol reaction with the starting ketone to form the corresponding α,β-unsaturated ketone, which finally is reduced through a Michael-type addition by the aforementioned ruthenium hydride intermediate.

Nitrones and Oxaziridines. XLII Synthesis of Indol-3-yl Substituted 1-Pyrroline 1-Oxides

The 1-pyrroline 1-oxides (13), (14), (16) and (18) with indol-3-yl substituents attached to the 2- or 4-positions have been synthesized by reductive cyclization of the related γ-nitro ketones.The corresponding 1-pyrrolines (15), (17) and (19) have also be