A chromeno[4,3-d]pyrazolo[3,4-b]pyridinone derivative 3 bearing thieno[2,3-d]pyrimidine moiety, 5-methyl-1-phenyl-3-(thieno[2,3-d]pyrimidin-4-yl)chromeno[4,3-d]pyrazolo[3,4-b]pyridin-6(3H)-one, was efficiently prepared in 75% yield by the reaction of 3-phenyl-1-(thieno[2,3-d]pyrimidin-4-yl)-1H-pyrazol-5-amine 1 with 3-acetyl-2H-chromen-2-one 2 presence FeCl3-SiO2 as a catalyst refluxing ethanol...

Abstract Anaplastic lymphoma kinase (ALK) is a promising target for the treatment of non-small cell lung cancer. Under crizotinib treatment, drug resistance and progressive disease appeared after point mutations arising in domain ALK. Second-generation ALK inhibitors can solve deficiencies first generation, especially cancer chemotherapy. Ceritinib (LDK378), pyrimidine derivative, example, inhi...

Two monoclinic (P21/c; Z′ = 1) polymorphs, α (from methanol) and β ethanol, n-propanol iso-propanol), of a bioactive pyrazolo[3,4-d]pyrimidine derivative have been isolated characterised by X-ray crystallography as well range computational chemistry techniques. The different conformations observed for the molecules in crystals are due to dictates molecular packing revealed geometry-optimisation...

A new pyrimidine derivative was prepared by reaction of Pyridimine-4,5-diaminewith 3-Phenyl propanal in good yield. This Schiff base characterized elemental analysis, Infra-red and Proton Nuclear Magnetic Resonance (1H- NMR) spectroscopy. The toxicity the compound also assayed via determination their LD50 value using Dixon method. novel 618.75 mg/Kg BW when administered Intraperitonially. In At...

Silver(I) coordination complexes with the versatile and biomimetic ligands 1,2,4-triazolo[1,5-a]pyrimidine (tp), 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine (dmtp) and 7-amine-1,2,4-triazolo[1,5-a]pyrimidine (7atp) all feature dinuclear [Ag(2)(μ-tp)(2)](2+) building units (where tp is a triazolopyrimidine derivative), which are the preferred motif, independently of the counter-anion used. Acco...

Pyrazofurin (NSC 143095) as the monophosphate derivative is a potent inhibitor of orotidine 5'-monophosphate (OMP) decarboxylase of the pyrimidine pathway and has been proposed to inhibit 5-aminoimidazole-4-carboxamide ribotide (AICAR) transformylase (EC 2.1.2.3) of the purine pathway (J. F. Worzalla, and M. J. Sweeney, Pyrazofurin inhibition of purine biosynthesis via 5-aminoimidazole-4-carbox...

In this study, a new series of 6-amino-1,3-dimethyluracil derivative with 6-(3-substituted N-benzylidene)-1,3-dimethyl pyrimidine-2,4-dione-6-yl derivatives which were synthesized by using one pot synthesis. The reaction and different aromatic aldehyde in ethanol yielded Schiff bases (1-6). the subsequent step )1-6) 2-mercaptoacetic acid, 2-chloroacetic acid 2-amino acetic acidn Tetrahydrofuran...

We explore the potential of the Diels-Alder cycloaddition for the functional tagging of DNA strands. A deoxyuridine triphosphate derivative carrying a diene at position 5 of the pyrimidine base was synthesized using a two-step procedure. The derivative was efficiently accepted as substrate in enzymatic polymerization assays. Diene carrying strands underwent successful cycloaddition with maleimi...

In earlier papers the presence of protein decomposition products in soils was reported and it was shown that in soils the changes occurring in the decay of such plant and animal materials as get into the soil are similar to the changes occuring under other conditions in the laboratory or in nature. The presence of arginine and histidine in soils was definitely established by isolating these deg...

Herein we describe NMR experiments and structural modifications of 4-methyl-2-phenylpyrimidine-N-acylhydrazone compounds (aryl-NAH) in order to discover if duplication of some signals in their ¹H- and ¹³C-NMR spectra was related to a mixture of imine double bond stereoisomers (E/Z) or CO-NH bond conformers (syn and anti-periplanar). NMR data from NOEdiff, 2D-NOESY and ¹H-NMR spectra at differen...