185408-97-3

Upstream product

• 62-53-3 aniline 
• 5451-40-1 2,6 dichloropurine 
• 97965-44-1 2-acetamido-9-acetyl-6-chloropurine 
• 73-40-5 2-amino-6-hydroxypurine 
• 10310-21-1 2-Amino-6-chloropurin 
• 5451-40-1 2,6-dichloro-7H-purine 

Downstream Products

• 903583-23-3 2-benzylamino-6-phenylamino-purine 
• 903583-25-5 2,5-anhydro-3,4-di-O-benzyl-1-(2-benzylamino-6-phenylamino-9H-purin-9-yl)-1-deoxy-D-glucitol 
• 903583-24-4 2,5-anhydro-3,4-di-O-benzyl-1-[2-(N,N-diethylamino-3-propylamino)-6-phenylamino-9H-purin-9-yl]-1-deoxy-D-glucitol 
• 1236431-97-2 N-phenyl-2-morpholino-9H-purin-6-amine 
• 1236432-16-8 N-phenyl-2-(4-(2-hydroxyethyl)piperazin-1-yl)-9H-purin-6-amine 
• 1338807-93-4 2-p-chloroaniline-6-anlilinepurine 
• 1338807-94-5 2-p-methoxyaniline-6-anlilinepurine 
• 52819-68-8 2,6-dianlilinepurine 
• 310401-64-0 2-chloro-9-cyclopentyl-N-phenyl-9H-purin-6-amine 
• 203436-33-3 2-chloro-9-isopropyl-N-phenyl-9H-purin-6-amine 

Relevant academic research and scientific papers

Pyrimido five-membered heterocyclic compound and application as mutant IDH2 inhibitor

The invention relates to a pyrimido five-membered heterocyclic compound and an application of the pyrimido five-membered heterocyclic compound as a mutant IDH2 inhibitor, and specifically discloses apyrimido five-membered heterocyclic compound capable of being used as a mutant IDH2 inhibitor, or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof. The invention also relates to a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in preparation of drugs for preventing and/or treating mutantIDH2 mediated diseases.

Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer

In the current study, we have designed and synthesized a series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative compound 14d with excellent antiproliferative activities towards five solid cancer cells, showed potent inhibitory activities against HDAC1, HDAC2 and CDK2 with IC50 values of 70.7 nM, 23.1 nM and 0.80 μM, respectively. Besides, compound 14d could effectively block the cell cycle in the G2/M phase and induce apoptosis, which might be related to increasing intracellular ROS levels. Importantly, compound 14d exhibited desirable pharmacokinetic (PK) properties with the intraperitoneal bioavailability of 50.8percent in ICR mice, and potent in vivo antitumor activity in the HCT116 xenograft model. Therefore, compound 14d could be considered as a promising lead compound for the development of multitargeting anticancer agents.

Syntheses and biological evaluation of novel hydroxamic acid derivatives containing purine moiety as histone deacetylase inhibitors

The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, th

Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases

Bacterial histidine kinases (HKs) are quintessential regulatory enzymes found ubiquitously in bacteria. Apart from their regulatory roles, they are also involved in the production of virulence factors and conferring resistance to various antibiotics in pathogenic microbes. We have previously reported compounds that inhibit multiple HKs by targeting the conserved catalytic and ATP-binding (CA) domain. Herein, we conduct a detailed structure-activity relationship assessment of adenine-based inhibitors using biochemical and docking methods. These studies have resulted in several observations. First, interaction of an inhibitor's amine group with the conserved active-site Asp is essential for activity and likely dictates its orientation in the binding pocket. Second, a N-NH-N triad in the inhibitor scaffold is highly preferred for binding to conserved Gly:Asp:Asn residues. Lastly, hydrophobic electron-withdrawing groups at several positions in the adenine core enhance potency. The selectivity of these inhibitors was tested against heat shock protein 90 (HSP90), which possesses a similar ATP-binding fold. We found that groups that target the ATP-lid portion of the catalytic domain, such as a six-membered ring, confer selectivity for HKs.

Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases

This study describes the discovery of novel dengue virus inhibitors targeting both a crucial viral protein-protein interaction and an essential host cell factor as a strategy to reduce the emergence of drug resistance. Starting from known c-Src inhibitors

Microwave assisted synthesis of 2,6-substituted aromatic-aminopurine derivatives

A series of novel 2, 6-diaromatic-aminopurines (6a-6t) have been synthesized from guanine and characterized fully. The effects of different catalysts on the N-alkylation of 2-position of purine ring were discussed.

N-Alkylation of 2,6-dichloropurine hydrochloride with a variety of alcohols over alumina catalyst

2,6-Dichloropurine hydrochloride reacts with various types of alcohols using different alumina catalysts and converts into its N-9-alkyl-2-chloro-6- hydroxy-9H-purine products to an extent of 49-74%. The product selectivity depends on the stability of carbocation generated from the alcohol. More stable carbocation formulates both N-7 and N-9-alkyl-2,6-dichloropurine products, whereas the less stable carbocation results in exclusively N-9-alkyl-2-chloro-6- hydroxy-9H-purine. The catalytic activity of alumina prepared using the sol-gel method has larger Brunauer, Emmett, and Teller (BET) surface area and hence shows significantly greater catalytic activity than the commercially available alumina samples. Copyright

SUBSTITUTED 6-ANILINOPURINE DERIVATIVES AS INHIBITORS OF CYTOKININ OXIDASE/DEHYDROGENASE AND PREPARATIONS CONTAINING THESE DERIVATIVES

The invention relates to substituted 6-anilinopurine derivatives of the general formula I, wherein R denotes one to five substituents independently selected from the group consisting of hydrogen, halogen, hydroxyl, amino, alkyloxy and alkyl group, and R2 denotes amino, halogen, nitro, thio, alkylthio or alkyl group for use as inhibitors of cytokinin oxidase/dehydrogenase. The invention also relates to the compositions containing these derivatives.

Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase

We report here the discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase by adopting a strategy integrating focused combinatorial library design, virtual screening, chemical synthesis, and bioass

Novel potent inhibitors of A. thaliana cytokinin oxidase/dehydrogenase

The synthesis of a new group of 2-X-6-anilinopurines, including compounds with potential cytokinin-like activities, with various substitutions (X = H, halogen, amino, methylthio or nitro) on the phenyl ring is described. The prepared compounds have been characterized using standard physico-chemical methods, and the influence of individual substituents on biological activity has been compared in three different bioassays, based on the stimulation of tobacco callus growth, retention of chlorophyll in excised wheat leaves and the dark induction of betacyanin synthesis in Amaranthus cotyledons. The biological activity of the prepared compounds was also assessed in receptor assays, in which the ability of the compounds to activate the cytokinin receptors AHK3 and AHK4/CRE1 was studied. Finally, the interactions of the compounds with the Arabidopsis cytokinin oxidase/dehydrogenase AtCKX2 (heterologously expressed) were investigated. Systematic testing led to the identification of two very potent inhibitors of AtCKX2: 2-chloro-6-(3-methoxyphenyl)aminopurine and 2-fluoro-6-(3-methoxyphenyl)aminopurine.