50614-86-3

Usage

Uses

Used in Pharmaceutical Industry:
Ethanone, 1-(1H-indol-4-yl)(9CI) is used as a precursor in the synthesis of various pharmaceutical drugs. Its unique chemical structure allows it to be a key component in the development of new medications with potential therapeutic benefits.
Used in Organic Chemical Reactions:
As a reagent, Ethanone, 1-(1H-indol-4-yl)(9CI) plays a crucial role in organic chemical reactions, facilitating the formation of desired products and aiding in the advancement of chemical research and development.
Used in Antiviral Applications:
Ethanone, 1-(1H-indol-4-yl)(9CI) has been studied for its potential antiviral properties, making it a candidate for further research and development as a therapeutic agent against viral infections.
Used in Anti-inflammatory Applications:
Ethanone, 1-(1H-indol-4-yl)(9CI) has also demonstrated anti-inflammatory properties, which could be harnessed for the development of treatments targeting inflammation-related conditions.
As research continues, additional applications and industries may be identified for Ethanone, 1-(1H-indol-4-yl)(9CI), further expanding its potential uses and contributions to various fields.

Upstream product

• 88059-19-2 trans-6-cyano-β-dimethylamino-2-nitrostyrene 
• 1074-86-8 4-formyl indole 
• 75-16-1 methylmagnesium bromide 
• 73805-13-7 1-(1H-indol-4-yl)ethan-1-ol 
• 84341-19-5 ethyl 4-acetyl-1H-indole-2-carboxylate 
• 84341-20-8 acetyl-4 carboxy-2 indole 
• 16136-52-0 4-cyanoindole 
• 917-54-4 methyllithium 

Downstream Products

• 88059-22-7 1-(t-butoxycarbonyl)-4-<1-hydroxy-2-(benzylmethylamino)ethyl>indole 
• 1425933-63-6 (+/-)-4-(1-bromoethyl)-1-tosyl-1H-indole 
• 112970-73-7 1-(1-tosyl-1H-indol-4-yl)ethanone 
• 120160-29-4 1-(1-methyl-1H-indol-4-yl)-ethanone 
• 188260-50-6 {4-[1-(3-Amino-propyl)-1H-indol-4-yl]-pyrimidin-2-yl}-[3-(1,1,2,2-tetrafluoro-ethoxy)-phenyl]-amine 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site

A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of these synthesized quinoline-indole derivatives have been intensively investigated. Two compounds 27c and 34b exhibited the most potent activities against five cancer cell lines with IC50 values ranging from 2 to 11 nM, which were comparable to those of Combretastatin A-4 (CA-4, 1). Further mechanism investigations revealed that 34b effectively inhibited the microtubule polymerization by binding to the colchicine site of tubulin. Further cellular mechanism studies elucidated that 34b disrupted cell microtubule networks, arrested the cell cycle at G2/M phase, induced apoptosis and depolarized mitochondria of K562 cells. Moreover, 34b displayed potent anti-vascular activity in both wound healing and tube formation assays. Importantly, 27c and 34b significantly inhibited tumor growth in H22 xenograft models without apparent toxicity, suggesting that 27c and 34b deserve further research as potent antitumor agents for cancer therapy.

SUBSTITUTED TRICYCLIC COMPOUNDS

Disclosed are compounds of the general formula (I), its tautomeric form, its stereoisomer, its pharmaceutically acceptable salt, its polymorph, or solvate thereof, Formula (I) wherein, ring A, R1 to R5, X, Y, m, and n are as defined herein, for use as SOS1 inhibitors in the treatment of proliferative, infectious and RASopathy diseases or disorders. Also disclosed are methods of synthesizing the compound of formula I, pharmaceutical compositions containing the compound of formula I, method of treatment of proliferative, infectious and RASopathy diseases or disorder, for example, a cancer, by administering the said compound and combinations of the compound of formula I with other active ingredients.

ROCK KINASE INHIBITORS

The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.

Quinoline substituted indole compound, and preparation method and application thereof

The invention discloses a quinoline substituted indole compound, a pharmaceutical composition containing the quinoline substituted indole compound, and a preparation method for the quinoline substituted indole compound. The invention also discloses the quinoline substituted indole compound, a pharmaceutical application for the pharmaceutical composition containing the quinoline substituted indolecompound, specifically an application of the pharmaceutical composition containing the quinoline substituted indole compound in preparation of drugs used for treatment of tumors, and an application ofthe quinoline substituted indole compound in preparation of drugs used for treatment of diseases or symptoms by inhibition of tubulin activity.

2-Aminoimidazole-based antagonists of the 5-HT6 receptor – A new concept in aminergic GPCR ligand design

A new strategy in the design of aminergic GPCR ligands is proposed – the use of aromatic, heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. This molecular switch may be responsible for the observed differences in 5-HT6R activity of the studied chemotypes with different amine-like fragments. Considering the multiple functionalization sites of the embedded guanidine fragment, diverse libraries were constructed, and the relationships between the structure and activity, metabolic stability, and solubility were established. Compounds from the N-(1H-imidazol-2-yl)acylamide chemotype (10a–z) exhibited high affinity for 5-HT6R and very high selectivity over 5-HT1A, 5-HT2A, 5-HT7 and D2 receptors (negligible binding), which was attributed to their very weak basicity. The lead compound in the series 4-methyl-5-[1-(naphthalene-1-sulfonyl)-1H-indol-3-yl]-1H-imidazol-2-amine (9i) was shown to reverse the cognitive impairment caused by the administration of scopolamine in rats indicating procognitive potential.

Acetylation of N-heteroaryl bromides via PdCl2/(o-tolyl) 3P catalyzed heck reactions

A new user-friendly and convenient method for the acetylation of N-heteroaryl bromides is described. This process is based on the palladium-catalyzed olefination of an N-heteroaryl bromide with butyl vinyl ether, followed by acid hydrolysis of the intermediate heteroaryl vinyl ether in situ. Isopropanol at 85°C, in the presence of K3PO 4·3H2O (2 equiv), PdCl2 (2 mol%) and (o-tolyl)3P (4 mol%), provided the best conditions, giving yields of N-heteroaryl bromides up to 75%. Georg Thieme Verlag Stuttgart.

Synthesis of indole-4-carboxaldehydes and 4-Acetylindole from N-alkyl-5-aminoisoquinolinium salts

N-Alkyl-5-aminoisoquinolinium salts (8a-d) are converted into indole-4-carboxaldehydes (1a-c) on heating in a two phase alkyl acetate-water system containing an excess of a 2:1 sodium bisulfite-sodium sulfite mixture, 4-Acetylindole 1e is prepared in the same way from 1-methyl-2-cyanomethylisoquinolinium bromide 8f.

Synthesis of 4-(4-Alkyl-2-morpholinyl)indoles

N-Substituted 4-(2-morpholinyl)indoles were prepared from 1-(t-butoxycarbonyl)-4-acetylindole (7) which was itself prepared from 4-cyanoindole.Bromination of ketone 7, followed by reaction with amines and subsequent sodium borohydride reduction, gave amin

Synthese d'(indolyl-3)-4 dihydro-2,5 furanonnes-2 hydrosolubles

Une cyclisation du type Dieckmann suivie d'une decarboxylation permet d'acceder directement aux (indolyl-3)-4 dihydro-2,5 furanonnes-2 acetylees ou non sur l'homocycle a partir des ethoxycarbonylacetoxyacetyl-3 indoles correspondants sans protection prealable de la position 1 du cycle indolique et du substituant acyle de l'homocycle.