663180-95-8

Usage

Molecular Weight

355.2 The molecular weight or molar mass of the compound, which is the mass of one mole of the substance.

Chemical Class

Pyrazole Derivatives A group of chemical compounds that are derived from the pyrazole ring system.

Ester Form

1-(3,4-dichlorophenyl)-5-hydroxy-3-(3-pyridinyl)-1H-pyrazole-4-ethanol The ester form of the compound, which is a chemical functional group consisting of a carbonyl group (C=O) with an organic group attached to the oxygen.

Main Use

Research Purposes in Pharmaceuticals The primary use of the compound is for research purposes in the field of pharmaceuticals.

Potential Biological Activities

Analgesic, Anti-inflammatory, Neuroprotective, and Anti-cancer The potential biological activities of the compound, which are the effects it may have on living organisms, including pain relief, reduction of inflammation, protection of nerve cells, and inhibition of cancer growth.

Further Research Needed

To fully understand its potential applications The statement that more research is needed to fully understand the potential applications of the compound.

Upstream product

• 19763-90-7 3,4-dichlorophenylhydrazine hydrochloride 
• 59578-61-9 3-nicotinoyl-dihydro-furan-2-one 
• 614-18-6 3-pyridinecarboxylic acid ethyl ester 

Downstream Products

• 663180-96-9 ethyl 4-((4-(2-acetoxyethyl)-1-(3,4-dichlorophenyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanoate 

Relevant academic research and scientific papers

Synthesis of structural analogues of GGT1-DU40, a potent GGTase-1 inhibitor

A series of new substituted pyrazoles 2-12 have been synthesized. The synthesized compounds are structural analogues of GGT1-DU40 1, a highly potent and selective inhibitor of protein geranylgeranyltransferase I (GGTase-I) both in vitro and in vivo. The i

Pyrazole-based potent inhibitors of GGT1: Synthesis, biological evaluation, and molecular docking studies

In this study, a series of pyrazole-based structural analogues of GGTI-DU40 (1) have been synthesized and biologically evaluated for geranylgeranyltransferase 1 (GGT1) and farnesyltransferase (FT) inhibition. The screening results revealed that 2 (IC50?=?2.4?μM) and 5 (IC50?=?3.1?μM) are potent GGT1 inhibitors (GGTIs), possessing higher inhibitory activity compared to the control compound 1 (IC50?=?3.3?μM). The anti-proliferative efficacy of these compounds was further assayed against MDA-MB-231?cells which indicated a significantly higher activity of 2 (IC50?=?7.6?μM) compared to 1 (IC50?=?23.0?μM). To examine the capacity of the synthesized compounds to inhibit GGT1 in an intact cell, western blot analysis was performed on the MDA-MB-231?cell line, which revealed very high inhibitory cellular activity of 2 and 5 and demonstrated their capacity to inhibit prenylation of endogenous proteins. Molecular docking studies of 2 against the crystal structure of GGT1 complexed with a geranylgeranyl pyrophosphate (GGPP) Analog and a CaaX (C?=?cysteine, aa?=?aliphatic amino acids, and X?=?any amino acid) portion of the KKKSKTKCVIL peptide substrate revealed several hydrogen bonding interactions and π-π contacts between 2 and the binding pocket of GGT1. Together these data suggest that compound 2 could proceed to in?vivo investigation to further assess its efficacy and cytotoxicity.

Prenylation inhibitors and methods of their synthesis and use

The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.