622381-65-1

Usage

Uses

Used in Pharmaceutical Research and Development:
[4-[(4-METHYLPIPERAZIN-1-YL)METHYL]PHENYL]METHANOL is used as a chemical compound in pharmaceutical research and development for its potential use in treating various neurological conditions and as an anti-cancer agent.
Used in Central Nervous System Depressant Applications:
[4-[(4-METHYLPIPERAZIN-1-YL)METHYL]PHENYL]METHANOL is used as a central nervous system depressant for its potential use in treating various neurological conditions.
Used in Anti-Cancer Applications:
[4-[(4-METHYLPIPERAZIN-1-YL)METHYL]PHENYL]METHANOL is used as a potential anti-cancer agent for its promising results in inhibiting the growth of certain cancer cells in vitro. Further research is needed to fully understand its potential therapeutic uses in this area.

InChI:InChI=1/C13H20N2O/c1-14-6-8-15(9-7-14)10-12-2-4-13(11-16)5-3-12/h2-5,16H,6-11H2,1H3

Upstream product

• 314268-40-1 4-((4-methylpiperazin-1-yl)methyl)-benzoic acid methyl ester 
• 1044872-32-3 4-(4-methyl piperazin-1-ylmethyl)-benzoic acid ethyl ester 
• 1571-08-0 methyl 4-formylbenzoate 
• 26496-94-6 Ethyl 4-(bromomethyl)benzoate 
• 109-01-3 1-methyl-piperazine 
• 2417-72-3 Methyl 4-(bromomethyl)benzoate 

Downstream Products

• 439691-80-2 4-((4-methylpiperazin-1-yl)methyl)benzaldehyde 
• 1323410-38-3 methyl 5-amino-4-(4-((4-((4-methylpiperazin-1-yl)methyl)benzyl)oxy)-1-oxoisoindolin-2-yl)-5-oxopentanoate 

Relevant academic research and scientific papers

3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer's Disease

One of the main obstacles toward the discovery of effective anti-Alzheimer drugs is the multifactorial nature of its etiopathology. Therefore, the use of multitarget-directed ligands has emerged as particularly suitable. Such ligands, able to modulate different neurodegenerative pathways, for example, amyloid and tau cascades, as well as cognitive and neurogenic functions, are fostered to come. In this respect, we report herein on the first class of BACE-1/GSK-3β dual inhibitors based on a 3,4-dihydro-1,3,5-triazin-2(1H)-one skeleton, whose hit compound 1 showed interesting properties in a preliminary investigation. Notably, compound 2, endowed with well-balanced potencies against the two isolated enzymes (IC50 of 16 and 7 μM against BACE-1 and GSK-3β, respectively), displayed effective neuroprotective and neurogenic activities and no neurotoxicity in cell-based assays. It also showed good brain permeability in a pharmacokinetic assessment in mice. Overall, triazinone derivatives, thanks to the simultaneous modulation of multiple points of the diseased network, might emerge as suitable candidates to be tested in in vivo Alzheimer's disease models.

Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy

Autophagy inhibition is emerging as a promising anticancer strategy. We recently reported that the circadian nuclear receptor REV-ERBβ plays an unexpected role in sustaining cancer cell survival when the autophagy flux is compromised. We also identified 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methylpiperazin-1-yl)methyl]phenol, 1 (ARN5187), as a novel dual inhibitor of REV-ERBβ and autophagy. 1 had improved cytotoxicity against BT-474 breast cancer cells compared to chloroquine, a clinically relevant autophagy inhibitor. Here, we present the results of structure-activity studies, based around 1, that disclose the first class of dual inhibitors of REV-ERBβ and autophagy. This study led to identification of 18 and 28, which were more effective REV-ERBβ antagonists than 1 and were more cytotoxic to BT-474. The combination of optimal chemical and structural moieties of these analogs generated 30, which elicited 15-fold greater REV-ERBβ inhibitory and cytotoxic activities compared to 1. Furthermore, 30 induced death in a panel of tumor cell lines at doses 5-50 times lower than an equitoxic amount of chloroquine but did not affect the viability of normal mammary epithelial cells.

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.

COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

PIPERAZINE BENZOTHIAZOLES AS AGENTS FOR THE TREATMENT OF CEREBRAL ISCHEMIC DISORDERS OR CNS DISORDERS

The present invention is related to piperazine benzothiazole derivatives, notably for use in the treatment and/or prophylaxis of cerebral ischemic disorders or CNS disorders. The present invention is furthermore related to methods of their preparation.