97693-22-6

Upstream product

• 14527-26-5 2-methylisothiourea sulphate 
• 123-11-5 4-methoxy-benzaldehyde 
• 105-56-6 ethyl 2-cyanoacetate 
• 70638-54-9 5-cyano-4-oxo-6-(4-methoxyphenyl)-2-thioxo-1,2,3,4-tetrahydropyrimidine 
• 74-88-4 methyl iodide 
• 147895-43-0 S-methylisothiourea hemisulphate 

Downstream Products

• 1018154-65-8 morpholinopyrimidine-5-carbonitrile 
• 1338916-90-7 1-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-D-glucopyranosyl)-5-cyano-6-(4-methoxyphenyl)-2-(methylthio)pyrimidin-4(1H)-one 
• 1338916-96-3 1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-5-cyano-6-(4-methoxyphenyl)-2-(methylthio)-pyrimidin-4(1H)-one 
• 1338916-99-6 1-(β-D-glucopyranosyl)-5-cyano-6-(4-methoxyphenyl)-2-(methylthio)-pyrimidin-4(1H)-one 
• 1338917-02-4 1-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl)-5-cyano-6-(4-methoxyphenyl)-2-(methylthio)-pyrimidin-4(1H)-one 
• 1338917-05-7 1-(β-D-galactopyranosyl)-5-cyano-6-(4-methoxyphenyl)-2-(methylthio)-pyrimidin-4(1H)-one 

Relevant academic research and scientific papers

Novel antiproliferative agents bearing morpholinopyrimidine scaffold as PI3K inhibitors and apoptosis inducers; design, synthesis and molecular docking

Two series of novel morpholinopyrimidine derivatives were synthesized and screened for their in-vitro cytotoxic activity against 60 tumor cell line by the National Cancer Institute, USA. The in-vitro cytotoxic IC50 values for the most active compounds 6e, 6g, and 6l against the most sensitive cell line leukemia SR were estimated (IC50 = 0.76, 13.59, and 4.37 uM, respectively). To investigate their PI3K enzyme inhibition activity, the assay was done on Class IA (α, β, & δ) isoforms. The IC50 values were very promising: compound [6e = 11.73 (α), 6.09 (β), 11.18 (δ)], compound [6g = 8.43 (α), 15.84 (β), 30.62 (δ)], and compound [6l = 13.98 (α), 7.22 (β), 10.94 (δ)], compared to the reference compound LY294002 = 6.28 (α), 4.51 (β), 4.60 (δ) uM, respectively. Moreover, cell cycle analysis and annexin V-FITC staining were done on Leukemia SR, there was arrest at G2/M phase and apoptosis was induced. Finally, docking study was performed to analyze the interactive mode of these derivatives in PI3Kα ATP-binding site. These outcomes proved that compounds 6e, 6g, and 6l are potential leads for further optimization as antileukemic agents.

Synthesis and Anti-HBV Activity of Novel Substituted Pyrimidine Glycosides and Their Acyclic Analogues

New aryl substituted uracil and thiouracil glycosides are synthesized by glycosylation at N1 in the pyrimidine nucleus using glycopyranosyl halides in basic medium. In addition C-linked hydrazinyl acyclic sugar derivatives exhibiting different

Vasoactive thiomethyl-pyrimidines: Promising drug candidates with vascular activity

Pyrimidines and their derivatives are present in various biologically active molecules. Most of the synthetic methods employed to achieve the pyrimidinone ring consist of two stages: The synthesis of a Michael intermediate from an aldehyde and an "active

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids

Abstract A series of hybrids comprising of 5-cyanopyrimidine and quinoline moiety were synthesized and tested for in vitro antiplasmodial activity against NF54 and Dd2 strains of Plasmodium falciparum. Hybrid bearing m-nitrophenyl substituent at C-4 of py

Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay

A series of novel pyrimidine analogues were synthesized and evaluated for immunosuppressive activity in the Mixed Lymphocyte Reaction assay, which is well-known as the in vitro model for in vivo rejection after organ transplantation. Systematic variation of the substituents at positions 2, 4 and 6 of the pyrimidine scaffold led to the discovery of 2-benzylthio-5-cyano-6-(4- methoxyphenyl)-4-morpholinopyrimidine with an IC50 value of 1.6 μM in the MLR assay.

An efficient and facile synthesis of inhibitors for hepatitis C viral and anti-SARS agents: 4-aryl-5-cyano-1,6-dihydro-2-thiouracils

One-pot, multicomponent reaction for the synthesis of 4-aryl-5-cyano-1,6- dihydro-2-thiouracils via three-component from aromatic aldehydes, ethyl 2-cyanoacetate and S-benzylisothiourea hydrochloride (methyl carbamimidothioate sulfate) under methanol is d

Synthesis and antiviral activity of new substituted pyrimidine glycosides

A number of N-substituted pyrimidine glycosides were synthesized by coupling reaction of the pyrimidine base with acetobromosugars followed by deprotection. The synthesized compounds were tested for their antiviral activity against Hepatitis B Virus (HBV). Plaque reduction infectivity assay was used to determine virus count reduction as a result of treatment with tested compounds which showed moderate to high anti viral activities.

Suitably functionalised pyrimidines as potential antimycotic agents

Various suitably functionalised pyrimidine derivatives have been synthesized to explore their potential as antimycotic agents. Some of the synthesized compounds 4c, 4d, 8a-e have shown highly significant in vitro antifungal activity against five human pathogenic fungi. (C) 2000 Elsevier Science Ltd. All rights reserved.

Glycosylation of 2-thiouracil derivatives. A synthetic approach to 3- glycosyl-2,4-dioxypyrimidines

Reaction of 6-aryl-5-cyano-2-thiouracils 2a-d with glycosyl halides 4a,b under alkaline conditions gave the respective bisglycosylated derivatives 5a- h. However, their deacetylation with ammonia in methanol caused a cleavage of the S-glycosyl residue and gave the N-3 glycosylated analogues 6a-h.

A One-Step Synthesis of 2-Methylthio-6-oxopyrimidine Derivatives: Preparation of Fused Pyrimidinones

Condensation of a ternary mixture of ethyl cyanoacetate, S-methylisothiourea and aromatic aldehydes in pyridine afforded directly the 4-aryl-5-cyano-6-oxopyrimidines IV in good yields.Alkylation of IV with alkyl halides in alkaline medium yielded the 1-al