Search results for "Pyrimidine"
showing 10 items of 589 documents
Synthesis and preliminary biological evaluation of a new pyridocarbazole derivative covalently linked to a thymidine nucleoside as a potential target…
2003
The therapy of human cancer is one of the more pursued goals by medicinal chemistry research. Most of the compounds clinically used as a treatment owe their efficacy to their cytotoxic interaction (direct or indirect) with nuclear DNA. This interaction results in the inhibition of DNA synthesis and the degradation of nucleic strands. Ellipticine is a naturally occurring 6H-pyrido[4,3-b]carbazole alkaloid endowed with antitumor activity, and several ellipticine derivatives have been used in clinical trials. We previously reported some 1,4-dimethyl-9H-carbazole derivatives structurally related to ellipticine. The purpose of our research was to transform the pyridocarbazole in a prodrug so tha…
Linear, tripodal, macrocyclic: Ligand geometry and ORR activity of supported Pd(II) complexes
2021
Abstract The novel ligand H3L designed to spontaneously adsorb onto MWCNT via electron-deficient pyrimidine residues and bind metal cations is used to prepare an oxygen reduction reaction (ORR) cathode catalyst based on supported Pd(II) complexes. Herein we report the synthesis of the ligand, its solution behaviour (protonation constants, binding constants for the test cation Cu(II), UV evidence of Cu(II) and Pd(II) complexes formation) and ORR performances together with XPS and STEM characterization. Tripodal nature of the H3L ligand frame it in-between previously studied macrocyclic and linear open chain ligands, allowing to draw meaningful comparisons.
Partial purification and some properties of a nucleoside phosphotransferase of chick embryos.
1978
A nucleoside phosphotransferase purified about 40fold from chick embryos utilizes efficiently as phosphate donors deoxyribonucleoside and pyrimidine ribonucleoside monophosphates, whereas the pyrimidine deoxyribonucleoside appear to be the preferred acceptors of phosphate. The enzyme is very unstable to heat, dilution and dialysis. A marked enhancement in the stability is caused by nucleotides and it seems associated with the formation of an aggregated state of the protein.
Organomercury(II) derivatives of 2-thiouracil. An infrared and proton magnetic resonance study of structures
1983
Abstract The novel complexes RHg(s2UraH−1) (R = Me, Ph) where s2UraH−1 is the monoanion of 2-thiouracil, have been synthesized. Comparison of the infrared spectra of the solid complexes and of 1H nuclear magnetic resonance spectra of the complexes in dimethyl-d6 sulfoxide with spectra of s2 Ura and Na[s2UraH−1] allows the recognition of the existence of isomers in the solid, with bonding to exocyclic sulfur and to pyrimidine nitrogens. In solution, a simpler pattern is observed, with 2J(1H199Hg) indicating bonding to sulfur only.
Syntheses, Mössbauer and infrared spectroscopic investigations on tin(II) chloride adducts with purine and pyrimidine bases and nucleosides
1982
Abstract The synthesis of two types of tin(II) complex SnCl2·L·CH3OH (L = adenosine, cytidine and inosine) and SnCl2·L2·CH3OH (L = adenine and cytosine) are described. The complexes are characterised by their infrared and 119Sn Mossbauer data. The Mossbauer shift data suggest that the bonds between tin(II) chloride and the donor atoms of the ligands are relatively weak.
High-dimensional malonate-based materials: Synthesis, crystal structures and magnetic properties of [M2(mal)2(L)(H2O)2]n·n(H2O) M = Zn(ii), Co(ii); H…
2003
Four novel coordination polymers [M2(mal)2(pym)(H2O)]n·nH2O, M = Zn (1), Co (2) and [M2(mal)2(pyz)(H2O)]n·nH2O, M = Zn (3), Co (4) (H2mal = malonic acid, pym = pyrimidine, pyz = pyrazine), have been synthesized. Compounds 1 and 2 are isomorphous, as are compounds 3 and 4. X-ray diffraction experiments reveal that 1–4 exhibit an interesting 3D-network, containing malonate and either pyrimidine (1 and 2) and pyrazine (3 and 4) as organic ligands. Variable-temperature magnetic susceptibility measurements indicate the occurrence of weak antiferromagnetic interactions between Co(II) ions in 2 and 4.
Surface-Enhanced Raman Study of the Interactions between Tripodal Cationic Polyamines and Polynucleotides
2011
Raman and surface-enhanced Raman spectra of new DNA/RNA-binding compounds consisting of three imidazole (Im) and three pyridine (Py) rings connected by tripodal polyaminomethylene linkages were obtained by the near-infrared excitation at 1064 nm. Study of interactions of Im and Py polyamines with single-stranded RNA polynucleotides (poly A, poly G, poly C, poly U), double-stranded DNA polynucleotides (poly dAdT-poly dAdT, poly dGdC-poly dGdC) and calf thymus DNA (ct-DNA) by surface-enhanced Raman spectroscopy (SERS) reveals unambiguous enhancement of the Raman scattering from the small molecules as well as appearance of new bands in spectra associated mainly with nucleobases. The SERS exper…
Elucidating the catalytic reaction mechanism of orotate phosphoribosyltransferase by means of X-ray crystallography and computational simulations
2020
15 p.-8 fig.-2 tab.1 graph. abst.+ 8 fig. supl.-1 tab. supl.
An unexpected Dimroth rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.
2013
An unusual Dimroth rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative …
New annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines, with potent anticancer activity, designed through VLAK protocol
2012
Drug design was performed through the Virtual Lock-and-Key (VLAK) protocol. This in silico approach allowed to select new annelated thienotriazolopyrimidine derivatives, potentially antitumor drugs. Starting from benzothieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine and Pyrido[3',2':4,5]thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core structures, new derivatives of these nuclei were designed and synthesized. Three of them were selected by the Development Therapeutical Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited an excellent antiproliferative act…