849513-58-2

Usage

Uses

Used in Pharmaceutical Research:
N-[4-(2,4,6-Trimethylphenyl)-2-thiazolyl]-4-pyridinecarboxamide is utilized as a research compound for exploring its potential biological activities and therapeutic effects. Its unique structure may offer novel avenues for drug discovery and development.
Used in Drug Development:
In the pharmaceutical industry, N-[4-(2,4,6-Trimethylphenyl)-2-thiazolyl]-4-pyridinecarboxamide serves as a lead compound for the design and synthesis of new drugs. Its molecular properties could be harnessed to target specific diseases or conditions, pending further research into its pharmacological profile.

Upstream product

• 4225-92-7 2-bromo-1-(2,4,6-trimethylphenyl)ethanone 
• 1667-01-2 2,4,6-Trimethylacetophenone 
• 55-22-1 pyridine-4-carboxylic acid 
• 81529-60-4 4-(2,4,6-trimethylphenyl)thiazol-2-ylamine 
• 108-67-8 1,3,5-trimethyl-benzene 
• 14254-57-0 4-(chlorocarbonyl)pyridine 

Relevant academic research and scientific papers

Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: Optimization of in vitro potencies and pharmacokinetic properties

A series of 4-aryl-N-arylcarbonyl-2-aminothiazoles of scaffold 4 was designed and synthesized as Hec1/Nek2 inhibitors. Structural optimization of 4 led to compound 32 bearing C-4′ 4-methoxyphenoxy and 4-(o-fluoropyridyl) carbonyl groups that showed low nanomolar in vitro antiproliferative activity (IC50: 16.3-42.7 nM), high intravenous AUC (64.9 μM·h, 2.0 mg/kg) in SD rats, and significant in vivo antitumor activity (T/C = 32%, 20 mg/kg, IV) in mice bearing human MDA-MB-231 xenografts. Cell responses resulting from Hec1/Nek2 inhibition were observed in cells treated with 32, including a reduced level of Hec1 coimmunoprecipitated with Nek2, degradation of Nek2, mitotic abnormalities, and apoptosis. Compound 32 showed selectivity toward cancer cells over normal phenotype cells and was inactive in a [ 3H]astemizole competitive binding assay for hERG liability screening. Therefore, 32 is as a good lead toward the discovery of a preclinical candidate targeting Hec1/Nek2 interaction.

Modulators Of HEC1 Activity And Methods Therefor

Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.