52177-08-9

Upstream product

• 2581-34-2 3-methyl-4-nitrophenol 
• 75-26-3 isopropyl bromide 
• 75-30-9 2-iodo-propane 

Downstream Products

• 676366-02-2 4-iso-propoxy-2-methylaniline 
• 1428641-81-9 diisopropyl1,2-bis(2-(5-isopropoxy-1-tosylindol-3-yl)ethyl)hydrazine-1,2-dicarboxylate 
• 1428641-80-8 C₂₈H₃₇N₃O₇S 
• 1428641-78-4 2-(5-isopropoxy-1-tosylindol-3-yl)ethyl methanesulfonate 
• 1428641-79-5 2-(5-isopropoxy-1-tosylindol-3-yl)ethanol 
• 1428641-85-3 3-(2-(tert-butyldimethylsilyloxy)ethyl)-5-isopropoxy-1-tosylindole 
• 396091-50-2 5-isopropoxy-1H-indole 
• 1335101-87-5 1-[(E)-2-(5-isopropoxy-2-nitrophenyl)vinyl]pyrrolidine 

Relevant academic research and scientific papers

INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE

Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').

INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE

The present disclosure is directed to compounds of formula I and methods of their use and preparation, as well as compositions comprising compounds of formula I.

Synthesis and biological evaluation of indolyl-pyridinyl-propenones having either methuosis or microtubule disruption activity

Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small molecules inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chemical substitutions at the 2-and 5-indolyl positions on our lead compound 3-(5-methoxy-2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propene-1-one (MOMIPP). We have identified a number of compounds that induce methuosis at similar potencies, including an interesting analogue having a hydroxypropyl substituent at the 2-position. In addition, we have discovered that certain substitutions on the 2-indolyl position redirect the mode of cytotoxicity from methuosis to microtubule disruption. This switch in activity is associated with an increase in potency as large as 2 orders of magnitude. These compounds appear to represent a new class of potent microtubule-active anticancer agents.

Synthesis, insecticidal activities and SAR of novel phthalamides targeting calcium channel

In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activities of title compounds against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of title compounds showed moderate to high activities at the tested concentration. The structure-activity relationship (SAR) was discussed in detail. During synthesizing title compounds B8, C7, D1, D9 and D12, their corresponding positional isomers (B8′, C7′, D1′, D9′ and D12′) were afforded, and their structures were confirmed by 2D NMR. The calcium-imaging technique was also applied to investigate the effects of compounds B2, B10, C4 and C5 on the intracellular calcium ion concentration ([Ca2+]i), which indicated that they released stored calcium ions from endoplasmic reticulum, which denoted that some compounds are potential modulators of the insect ryanodine receptor (RyR).

Studies towards the synthesis of montamine: Synthesis of the 1,2-bis(indolyl)ethylhydrazine fragment

The synthesis of a protected 1,2-bis(indolyl)ethylhydrazine bearing the full substitution pattern present in the unusual dimeric alkaloid montamine is described. A variant of the Mitsunobu reaction was used to incorporate directly the reduced azodicarboxy

LRRK2 INHIBITORS

Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.

The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.

A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonist described so far (EC50 = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, Ki = 12 nM) to and 300-fold higher (1h, Ki = 0.04 nM) than serotonin.