113997-58-3

Upstream product

• 1201-26-9 3-(1H-indolyl)acetone 
• 3886-69-9 (R)-1-phenyl-ethyl-amine 
• 4771-72-6 α-methyl-β-(3-indolyl)-1-nitroethane 

Downstream Products

• 7795-52-0 (-)-alpha-Methyltryptamine 

Relevant academic research and scientific papers

REGIMENS OF ESTROGEN RECEPTOR ANTAGONISTS

Provided herein are methods of administering estrogen receptor antagonists for use in treatment of cancer. The antagonists (such as a hexahydro pyrido[3,4-b]indole, AZD9496, RAD-1901, ARN-810, endoxifen, or fulvestrant) may be an inhibitor of both activating function 1 and activating function 2 of the estrogen receptor. Also provided are combinations of above inhibitors with a secondary agent, which is a CDK 4/6 inhibitor (such as, palbocociclib, ribociclib, abemaciclib, lerociclib, and trilaciclib).

METHODS OF TREATING ESTROGEN RECEPTOR-ASSOCIATED DISEASES

The present disclosure provides methods of treating estrogen receptor-associated diseases, disorders, and conditions.

TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS

The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.

Synthesis and serotonin receptor affinities of a series of enantiomers of α-methyltryptamines: Evidence for the binding conformation of tryptamines at serotonin 5-HT(1B) receptors

A procedure for the preparation of optically pure α-methyltryptamines (AMTs) from substituted indoles was developed. The key step in the sequence was the reductive amination of substituted indole-2-propanones with the commercially available pure enantiomers of α-methylbenzylamine, followed by the chromatographic separation of the resulting pair of diastereomeric amines by preparative centrifugal (Chromatotron) chromatography. Catalytic N-debenzylation then afforded the pure AMT enantiomers. Optical purity was established by chiral HPLC analysis of the 2-naphthoylamide derivatives. An improved procedure for the preparation of indole-2-propranone was also developed. To probe structure-activity relationships of serotonin receptors, affinities of the α-methyltryptamine enantiomers were then measured at the 5-HT2 antagonist receptor subtype, with displacement of [3H]ketanserin, and were estimated at the 5-HT(1B) receptor, with displacement of [3H]serotonin, respectively, in rat frontal cortex homogenates. Enantioselectivity at the receptor subtypes varied, depending on aromatic substituents. For a 5-hydroxy or 5-methoxy, the S enantiomer had higher affinity or was equipotent to the R enantiomer. This selectivity at [3H]serotonin binding sites was reversed for 4-oxygenated α-methyltryptamines, where a 4-hydroxy or 4-methoxy did not enhance affinity over the unsubstituted compounds. These results can be explained, for the [3H]serotonin displacement data, if the binding conformation is one where the ethylamine side chain is trans and lying in a plane perpendicular to the indole ring plane.