51834-67-4

Upstream product

• 18370-81-5 (3-bromopropyl)amine 
• 108-24-7 acetic anhydride 
• 5003-71-4 3-bromopropylamine hydrochloride 
• 75-36-5 acetyl chloride 
• 41236-20-8 3-bromopropan-1-amine hydrochloride 

Downstream Products

• 208724-68-9 N-acetyl-N'-(p-chlorophenyl)-1,3-diaminopropane 
• 224314-00-5 1-(4-chloro-phenyl)-2-methyl-1,4,5,6-tetrahydro-pyrimidine 
• 78273-74-2 N-(3-{3-[(1-piperidyl)methyl]phenoxy}propyl)acetamide 

Relevant academic research and scientific papers

Investigation of B,C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors for use as anti-breast cancer agents

On the basis of deguelin, a series of the B,C-ring truncated surrogates with N-substituted amide linkers were investigated as HSP90 inhibitors. The structure activity relationship of the template was studied by incorporating various substitutions on the nitrogen of the amide linker and examining their HIF-1α inhibition. Among them, compound 57 showed potent HIF-1α inhibition and cytotoxicity in triple-negative breast cancer lines in a dose-dependent manner. Compound 57 downregulated expression and phosphorylation of major client proteins of HSP90 including AKT, ERK and STAT3, indicating that its antitumor activity was derived from the inhibition of HSP90 function. The molecular modeling of 57 demonstrated that 57 bound well to the C-terminal ATP-binding pocket in the open conformation of the hHSP90 homodimer with hydrogen bonding and pi-cation interactions. Overall, compound 57 is a potential antitumor agent for triple-negative breast cancer as a HSP90 C-terminal inhibitor.

Bromo-tyrosine alkaloidal compound as well as preparation method and application thereof

The invention belongs to the field of a medical technology, and concretely relates to a bromo-tyrosine alkaloidal compound as well as a preparation method and application thereof. The invention provides the bromo-tyrosine alkaloidal compound as shown in a general formula I and a general formula II, the preparation method thereof, and the application thereof in preparing an antitumor drug for the first time. The bromo-tyrosine alkaloidal compound has good antineoplastic activity, the preparation method is simple and feasible, the yield is better, and the bromo-tyrosine alkaloidal compound has abroad application prospect.

An acyl-SAM analog as an affinity ligand for identifying quorum sensing signal synthases

N-Acylhomoserine lactones (AHLs) are quorum sensing signals produced by Gram-negative bacteria. We here report the affinity purification of AHL synthases using beads conjugated with an enzyme inhibitor, which was designed based on the catalytic intermediate acyl-SAM. the Partner Organisations 2014.

PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS

The present invention relates to compounds II useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.

Synthesis and isolation of 5,6-dihydro-4 H -1,3-oxazine hydrobromides by autocyclization of N -(3-bromopropyl)amides

5,6-Dihydro-4H-1,3-oxazine hydrobromides have been synthesized by the nucleophilic autocyclo-O-alkylation of N-(3-bromopropyl)amides under neutral conditions in chloroform. It is found that electron-donating amide α-substituents influence the autocyclizat

Synthesis and properties of 1-aryl-2-alkyl-1,4,5,6- tetrahydropyrimidines

A general method is described for the synthesis of 1-aryl-2-alkyl- 1,4,5,6-tetrahydropyrimidines 1, by cyclization of N-acyl-N'- aryltrimethylenediamines 2 with trimethylsilyl polyphosphate. Precursors 2 were obtained by aminolysis of the corresponding N-(3-bromopropyl)arnides 3. The 1H nmr spectra of tetrahydropyrimidines 1 are analyzed, discussing the influence of substituents in positions 1 and 2 of the heterocyclic ring. Alkaline hydrolysis of compounds 1, which originates exclusively N-acyl-N'- aryltrimethylenediamines 2, through an intermediate carbinolamine, was also studied. Cleavage of such an intermediate is discussed in the light of the stereoelectronic control theory. Reduction of compounds 1 with borane, leads regiospecifically to N-alkyl-N'-aryltrimethylenediamines 6.