65389-77-7

Usage

InChI:InChI=1/C9H11ClN2O/c10-8-4-2-1-3-7(8)9(13)12-6-5-11/h1-4H,5-6,11H2,(H,12,13)

Upstream product

• 67333-74-8 1-(2-chloro-benzoyl)-1H-imidazole 
• 107-15-3 ethylenediamine 
• 333-18-6 1,2-diaminoethane dihydrochloride 
• 118-91-2 ortho-chlorobenzoic acid 

Downstream Products

• 83019-53-8 2-Chloro-N-[2-(2-hydroxy-3-phenoxy-propylamino)-ethyl]-benzamide 

Relevant academic research and scientific papers

A N, 6 diphenyl-pyrimidin-4-amine Bcr-Abl inhibitor and its preparation method and application

The invention discloses N,6 diphenylpyrimidine-4-amine Bcr-Abl inhibitors as well as a preparation method and application thereof. A structural formula of the inhibitors is shown in the specification, wherein in the structural formula, R is a mono-substituent or a di-substituent, and the substituent is alkyl, halogen or tertiary amino. The series of inhibitors have a certain inhibiting effect on ABL1 kinase in vitro, can inhibit tumor cell proliferation and can be used for preparing antitumor drugs, especially CML (chronic myelocytic leukemia) drugs. The preparation method of the N,6 diphenylpyrimidine-4-amine Bcr-Abl inhibitors, which is provided by the invention, has the advantages of easiness in obtainment of raw materials, mild reaction conditions, simplicity in operation of reaction processes and cheap used reagents.

Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib

In order to expand the structural diversity of Bcr-Abl inhibitors, twenty hybrids (series E and P) have been synthesized and characterized based on Imatinib and GNF-2. Their biological activities were evaluated in vitro against human leukemia cells. Most compounds exhibited potent antiproliferative activity against K562 cells, especially for compounds E4, E5 and E7. Furthermore, these new hybrids were also screened for Abl kinase inhibitory activity, and some of them inhibited Abl kinase with low micromolar IC50 values. In particular, compound P3 displayed the most potent activity with IC50 value of 0.017 μM comparable with that of Imatinib. Molecular docking studies indicated that these novel hybrids fitted well with the active site of Bcr-Abl. These results suggested the great potential of these compounds as novel Bcr-Abl inhibitors.

TRIAZOLE DERIVATIVE OR SALT THEREOF

[Problem] There is provided a compound which can be used for therapy of diseases in which 11 β-hydroxysteroid dehydrogenase type 1(11β-HSD1) participates, in particular diabetes, insulin resistance. [Means for Solution] It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11β-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance.