345264-52-0

Usage

General Description

1H-Indole-7-ethanol, also known as tryptophol, is a chemical compound with the molecular formula C10H9NO. It is a derivative of the amino acid tryptophan and is produced during the fermentation of various substances by certain microorganisms. Tryptophol has been found in alcoholic beverages such as beer and wine, as well as in the human body as a metabolite of tryptophan. It has been studied for its potential effects on the central nervous system, including its role in modulating mood and behavior. Tryptophol is also used in laboratory research as a precursor to other indole-derivative compounds with diverse biological activities.

Upstream product

• 94239-08-4 7-ethenyl-1H-indole 
• 408354-47-2 7-[2-(tert-butyldimethylsilanyloxy)ethyl]-1H-indole 
• 15121-84-3 2-nitro-benzeneethanol 
• 1074-88-0 1H-indole-7-carbaldehyde 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation

The efficacy of EGFR inhibitors is frequently affected by acquired resistance. EGFR19D/T790M/C797S mutation is one of the primary reasons for the emergence of resistance after treatment with the third-generation EGFR inhibitors such as AZD9291, CO1686 and Olmutinib. To overcome the resistance mutation 19D/T790M/C797S, we designed and prepared a series of indole derivatives with the terminal hydroxyl of alkyl chain to increase extra interaction with the Asp855 in the conservative DFG site. Activity evaluation, structure-activity relationship and docking analysis were also carried out. Among them, compound 12e displayed significant inhibitory activity against EGFR19D/T790M/C797S (IC50 = 15.3 nM) and good selectivity over EGFR WT (IC50 > 1000 nM), L858R/T790M (IC50, 156.6 nM) and L858R/T790M/C797S (IC50, 218.3 nM) respectively. Furthermore, 12e exhibited good growth inhibition activity, induced G1 phase cell cycle arrest and apoptosis in BaF3/EGFR19D/T790M/C797S cells by suppressing EGFR phosphorylation signaling pathway. In all, our study might provide a novel structural design method and lay the solid foundation for the development of the 4th generation EGFR19D/T790M/C797S inhibitors.

Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors

3-Acyl-indole derivative 1 was identified as a novel dengue virus (DENV) inhibitor from a DENV serotype 2 (DENV-2) phenotypic antiviral screen. Extensive SAR studies led to the discovery of new derivatives with improved DENV-2 potency as well as activity in nanomolar to micromolar range against the other DENV serotypes. In addition to the potency, physicochemical properties and metabolic stability in rat and human microsomes were improved during the optimization process. Chiral separation of the racemic mixtures showed a clear preference for one of the two enantiomers. Furthermore, rat pharmacokinetics of two compounds will be discussed in more detail, demonstrating the potential of this new series of pan-serotype-DENV inhibitors.

Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors

The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.

KINASE INHIBITORS

The present invention provides kinase inhibitors of Formula (I)

PURINE DERIVATIVES AS KINASE INHIBITORS

The present invention provides kinase inhibitors of Formula I.