38119-33-4

Upstream product

• 74-87-3 methylene chloride 
• 10310-21-1 2-Amino-6-chloropurin 
• 74-88-4 methyl iodide 

Downstream Products

• 7329-79-5 2-amino-6-mercapto-7-methylpurine 
• 116137-82-7 O⁶,7-dimethylguanine 
• 104802-81-5 2-amino-6-methylthio-7-methylpurine 

Relevant academic research and scientific papers

Regioselective alkylation reaction of purines under microwave irradiation

The alkylation of purines which is generally carried out after anion formation by treatment with a base and alkyl halide is complicated and in the best cases, mixtures of N-alkylated compounds are obtained. Purine derivatives can be acquired from alkylati

The discovery of purine-based agents targeting triple-negative breast cancer and the αB-crystallin/VEGF protein–protein interaction

Oestrogen receptor-negative breast cancer, particularly subtypes such as triple-negative breast cancer (TNBC, around 10–15% of cases), are characterised by poor long-term survival, poor response to therapy and early progression to metastasis. Purine-based compounds represent a privileged scaffold in anticancer drug design, with several clinically approved and experimental agents in clinical development comprising a purine core structure. In this study, a series of new purine-based compounds were synthesised; seven of the new analogues were found to significantly reduce the in vitro viability of TNBC cell lines (MDA-MB-231 and MDA-MB-436) with IC50 values of ≤50 μM. In previous work, we have proposed a new concept for targeting angiogenesis driving TNBC progression, by disrupting the protein–protein interaction between the molecular chaperone αB-crystallin (CRYAB) and VEGF. Since previous clinical studies applying anti-VEGF therapy to TNBC patients have met with limited success, we were interested to test our most promising purine analogues against CRYAB/VEGF, using a custom-designed cell-based CRYAB/VEGF165 interaction assay platform. Analogues 4e and 4f significantly reduced the interaction between CRYAB/VEGF165, and compound 4e (100 μM) was also found to decrease the levels of soluble VEGF expressed by MDA-MB-231 cells by 40%. In conclusion, these promising early activity profiles warrant further investigation to validate this concept.

Tricyclic purine analogs derived from 2-amino-6-chloropurine and 2,6-diaminopurine and their methylated quaternary salts

A novel series of tricyclic, etheno-bridged purine analogs was sythesized from 2-amino-6-(substituted amino)-9-methylpurines by cyclization with chloroacetaldehyde, with particular focus on the regioselectivity of the cyclization reaction and fluorescence properties. The analogs as well as the starting purines were alkylated with iodomethane, affording a new class of quaternary salts with potential biological activity. Neither significant fluorescence nor cytostatic effect was found.

HIV REPLICATION INHIBITING PURINE DERIVATIVES

The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula (I) a N-oxide, a pharmaceutically a

Synthesis of heteromine C from guanine

Heteromine C previously isolated from a Taipei folk medicine plant, has been synthesised for the first time by selective methylation reactions starting from guanine. Thermal rearrangement to 1-methylherbipoline takes place when heteromine C is heated. It is shown that treatment of O6,9- dimethylguanine with methyl iodide gives the O6,7,9-trimethylguaninium iodide with complete selectivity, while similar reaction on O6,7- dimethylguanine results in methylation both in the 3- and 9-position.