26175-40-6

Upstream product

• 937-53-1 (Z)-4-phenylbut-3-en-2-one 
• 17356-08-0 thiourea 
• 57626-32-1 2-amino-4-phenacylthiazole 
• 57626-31-0 1-phenyl-4-bromo-1,3-butanedione 
• 20845-80-1 1-chloro-4-phenylbutan-2-one 
• 1896-62-4 (E)-benzalacetone 
• 6310-44-7 3,4-dibromo-4-phenylbutan-2-one 

Downstream Products

• 103505-79-9 5-methyl-4-[(4-phenethyl-thiazol-2-ylamino)-methyl]-2-phenyl-1,2-dihydro-pyrazol-3-one 
• 99989-82-9 4-phenethyl-5-thiocyanato-thiazol-2-ylamine 
• 102316-56-3 (3-oxo-3-phenyl-propyl)-(4-phenethyl-thiazol-2-yl)-amine 
• 57634-53-4 5-chloro-4-phenethyl-thiazol-2-ylamine 

Relevant academic research and scientific papers

Derives de l'imidazothiazole X. Proprietes fongistatiques de 2-aminothiazoles et de 6-aryl imidazothiazoles substitues respectivement en 4 et en 3 par un reste arylethyle, aroylmethyle, β-hydroxy β-arylethyle et ethoxycarbonylmethyle

Several 2-aminothiazoles, substituted in 4 with an ethylacetate, aroylmethyl, β-hydroxy β-arylethyl or arylethyl chain, were combined with ω-bromoacetophenones in order to obtain the corresponding 3-substituted 6-arylimidazothiazoles to perform fun

Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity

We found that aminothiazole derivative (E)-N-(5-benzylthiazol-2-yl)-3-(furan-2-yl)acrylamide (1) has strong anticancer activity, and undertook proteomics approaches to identify the target protein of compound 1, importin β1 (KPNB1). A competitive binding assay using fluorescein-labeled 1 showed that 1 has strong binding affinity for KPNB1 (Kd: ～20 nm). Furthermore, through western blotting assays for KPNB1, KPNA2, EGFR, ErbB2, and STAT3, we confirmed that 1 has inhibitory effects on the importin pathway. KPBN1 appears to be overexpressed in several cancer cells, and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, while leaving non-cancerous cells unaffected. Therefore, compound 1 is a promising new lead for the development of KPNB1-targeted anticancer agents. Fluorescein-labeled 1 could be a useful quantitative probe for the development of novel KPNB1 inhibitors.

Imidazothiazole derivatives. XI. Modulation of the CD2-receptor of human T trypsinized lymphocytes by several imidazothiazoles

About 40 substituted imidazothiazoles were obtained in order to study their in vitro immunological effect on the modulation of the expression of human T trypsinized lymphocytes by the CD2 receptor.A synthetic program was developed to introduce either an oxygenated function, such as ester (11, 14), acid (12) and arylketonic groups (9, 13, 15), or two groups, such as an aryl and an ester (1, 6, 8), an acid (3, 7) or a hydrazide (2).These compounds were examined by an E-rosette-forming-cell test, and display a positive drug efficacity index, suggesting a regeneration effect on the expression of CD2 receptors.The following structural parameters are favourable: an aryl moiety on the C-6 with a methoxy or nitro group: and an ethyl ester on the C-3, a double bond to the 2,3-position (the 5,6-position is ineffective).Acid and hydrazide functions or the loss of phenyl group on the C-6 decrease this activity.If the aryl group is on the C-3 or C-2 side chain, the activity is weaker and more so for the latter.However, the most interesting derivatives are less immunostimulating than levamisole hydrochloride. immunomodulator / imidazothiazole / human T lymphocyte / CD2 receptor