54748-09-3

Upstream product

• 62-53-3 aniline 
• 49845-33-2 2,4-Dichloro-5-nitropyrimidine 

Downstream Products

• 102495-66-9 5-nitro-N⁴-phenyl-pyrimidine-2,4-diyldiamine 
• 89660-19-5 2-chloro-N⁴-phenylpyrimidine-4,5-diamine 
• 842129-23-1 N²-(4-(4-methylpiperazin-1-yl)phenyl)-5-nitro-N⁴-phenylpyrimidine-2,4-diamine 
• 1414781-16-0 C₂₈H₂₈N₈ 
• 842129-20-8 intermediate 18 
• 1144044-97-2 N₂-cyclopropyl-5-nitro-N₄-phenylpyrimidine-2,4-diamine 
• 89743-87-3 2-chloro-7-methyl-9-phenyl-7,9-dihydro-8H-purin-8-one 
• 89660-30-0 2-chloro-9-phenyl-7,9-dihydro-8H-purin-8-one 

Relevant academic research and scientific papers

Pyrimido azacyclo compound and application thereof

The invention discloses a pyrimido azacyclo compound represented by a general formula I, and a pharmaceutically acceptable salt thereof, and relates to the technical field of organic chemistry, wherein substituent groups X and Ar are defined in the specification. The invention also relates to application of the compound represented by the general formula I and the pharmaceutically acceptable saltthereof in medicines for treating diseases caused by abnormal high expression of URAT1, particularly in preparation of medicines for treating and/or preventing gout, wherein the general formula I is defined in the specification.

Inhibitor containing fused ring derivative as well as preparation method and application thereof

The invention relates to an inhibitor containing fused ring derivative as well as a preparation method and application thereof. Particularly, the invention relates to a compound as shown in a generalformula (I), a preparation method thereof, a pharmaceuti

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a]pyridin-6-yl)amino]-9-(tetrahydro-2 H-pyran-4-yl)-7,9-dihydro-8 H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

DNA-PK is a key component within the DNA damage response, as it is responsible for recognizing and repairing double-strand DNA breaks (DSBs) via non-homologous end joining. Historically it has been challenging to identify inhibitors of the DNA-PK catalyti

Purine series derivative, and preparation method and applications thereof

The invention discloses a purine series derivative represented by formula I, or a stereochemical isomer, a solvate, or a pharmaceutically acceptable salt of the purine series derivative, and also discloses a preparation method and applications of the comp

Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors

Pin1 (Protein interacting with NIMA1) is a cis–trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidi

Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold

Based upon the modeling binding mode of marketed AZD9291 with T790M, a series of N-9-Diphenyl-9H-purin-2-amine derivatives were designed and synthesized with the purpose to overcome the drug resistance resulted from T790M/L858R double mutations. The most potent compound 23a showed excellent enzyme inhibitory activities and selectivity with nanomolar IC50 values for both the single T790M and double T790M/L858R mutant EGFRs, and was more than 8-fold selective for wild type EGFR. Compound 23a displayed strong antiproliferative activity against the H1975 non-small cell lung cancer (NSCLC) cells bearing T790M/L858R. And it was less potent against A549 (WT EGFR and k-Ras mutation) and HT-29 (non-special gene type) cells, showing a high safety index.

Structural optimization and structure-activity relationships of N 2-(4-(4-methylpiperazin-1-yl)phenyl)- N 8-phenyl-9 H -purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations

This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine- 2,8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure-activity relationship studies led to the identification of 9-cyclopentyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N 8-phenyl-9H-purine-2,8-diamine (9e) that exhibits significant in vitro antitumor potency against the non-small-cell lung cancer (NSCLC) cell lines HCC827 and H1975, which harbor EGFR-activating and drug-resistance mutations, respectively. Compound 9e was further assessed for potency and selectivity in enzymatic assays and in vivo anti-NSCLC studies. The results indicated that compound 9e is a highly potent kinase inhibitor against both EGFR-activating and resistance mutations and has good kinase spectrum selectivity across the kinome. In vivo, oral administration of compound 9e at a dose of 5 mg/kg caused rapid and complete tumor regression in a HCC827 xenograft model, and an oral dose of 50 mg/kg initiated a considerable antitumor effect in an H1975 xenograft model.

Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury

In this Letter we describe the optimization of an aminopurine lead (1) with modest potency and poor overall kinase selectivity which led to the identification of a series of potent, selective JNK inhibitors. Improvement in kinase selectivity was enabled by introduction of an aliphatic side chain at the C-2 position. CC-359 (2) was selected as a potential clinical candidate for diseases manifested by ischemia reperfusion injury.

Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists

A series of trisubstituted purinones was synthesized and evaluated as A2A receptor antagonists. The A2A structure-activity relationships at the three substituted positions were studied and selectivity against the A1 recept