author={Ljubica Glava{\vs}-Obrovac and Ivan Karner and Marina Pavlak and Marko Rada{\vc}i{\'c} and Jelena Ka{\vs}nar-{\vS}amprec and Biserka Žini{\'c}},
  journal={Nucleosides, Nucleotides \& Nucleic Acids},
  pages={557 - 569}
Large-scale preparation of 5-bromo-1-mesyluracil (BMsU) 4 has been optimized. BMsU was synthesized by condensation of silylated 5-bromouracil and MsCl in acetonitrile or by the reaction of 5-bromouracil with MsCl in pyridine. The same product was obtained by bromination of 1-mesyluracil. The purpose of this study was to elucidate the effects of BMsU on the biosynthetic activity of tumor cell enzymes involved in DNA, RNA and protein syntheses, and in de novo and salvage pyrimidine and purine… 
9 Citations
Antiproliferative and proapoptotic activity of molecular copper(II) complex of N-1-tosylcytosine.
In vivo toxicity study of N-1-sulfonylcytosine derivatives and their mechanisms of action in cervical carcinoma cell line
SummaryNew N-1-sulfonylpyrimidines showed potent growth inhibitory activity against human and mouse tumour cells of different origin. 1-(p-toluenesulfonyl)cytosine (TsC) and
5‐Triazolyluracils and Their N1‐Sulfonyl Derivatives: Intriguing Reactivity Differences in the Sulfonation of Triazole N1′‐Substituted and N1′‐Unsubstituted Uracil Molecules
We describe the synthesis of novel C5-triazolyl derived N1-sulfonylpyrimidines through Cu(I)-catalyzed alkyne–azide cycloaddition followed by sulfonylation of the formed C5-triazolyl derivatives with
ESI-MS studies of the non-covalent interactions between biologically important metal ions and N-sulfonylcytosine derivatives.
The aim of this report is to present the electrospray ionization mass spectrometry results of the non-covalent interaction of two biologically active ligands, N-1-(p-toluenesulfonyl)cytosine, 1-TsC,
The transformation from 2°-amine to 3°-amine of cyclam ring alters the fragmentation patterns of 1-tosylcytosine-cyclam conjugates.
It was shown that the structure of the cyclam conjugate dictates the fragmentation reactions and not the metal ions.
Carbonic anhydrase inhibitory properties of some uracil derivatives
All compounds used in the study act as competitive inhibitors with substrate, 4-NPA, which are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine.
C5-Morpholinomethylation of N1-sulfonylcytosines by a one-pot microwave assisted Mannich reaction.
A fast and efficient route for the introduction of a methylene bridged-amine (morpholinomethyl) functionality in the C5 position of the sulfonylated cytosine nucleobase has been developed and peculiar tosyl-urea derivative 9 has been isolated, which provided additional insight into the reaction pathway.
N-sulfonylpyrimidine derivatives and hyperthermia treatment of anaplastic mammary carcinoma in vivo.
The aim of this study was to investigate in vivo antitumor activity of newly synthesized N-sulfonylpyrimidine derivatives applied as a single agent and in combination with hyperthermia (43 oC/60


5-(1-Adamantyl) pyrimidines as inhibitors of folate metabolism.
It appears that the adamantyl group in position 5 greatly facilitates the passage of pyrimidines through the plasma membrane of the cells, thereby increasing the inhibitory potency of these compounds in cellular systems over and above that expected from enzyme inhibition analysis.
Elucidation of pathways of 5-fluorouracil metabolism in xenografts of human colorectal adenocarcinoma.
Mode of action of the antitumor compound bruceantin, an inhibitor of protein synthesis.
It is demonstrated that the side chain of bruceantin is important for transport of the drug into intact cells and that partial unsaturation in ring A is required for inhibition of protein synthesis.
The influence of methotrexate pretreatment on 5-fluorouracil metabolism in L1210 cells.
Metabolism and ribonucleotide reductase inhibition of (E  )-2′-deoxy-2′-(fluoromethylene)cytidine, MDL 101,731, in human cervical carcinoma HeLa S3 cells
It is suggested that the prolonged ribonucleotide reductase inhibition by rapidly activated metabolites of MDL 101,731 in part contributes to the potent antitumor activity of this drug against various xenografts.
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
A series of diarylsulfonylureas with exceptionally broad-spectrum activity against syngeneic rodent solid tumors in vivo is described, and one compound from the series has progressed to Phase I clinical trials as an antitumor drug.
Inhibitory effects of fluorinated pyrimidines, 5¢-DFUR, UFT and T-506, in a model of hepatic metastasis of mouse colon 26 adenocarcinoma - assessment of inhibitory activity and adverse reactions at the maximum tolerated dose
5¢-DFUR and T-506 showed the highest rate of inhibition of hepatic metastasis, suggesting that these drugs would be effective for the prophylactic treatment of metastatic disease.
Thymidylate synthase inhibition after administration of fluorouracil with or without leucovorin in colon cancer patients: implications for treatment with fluorouracil.
Residual and total TS activity are predictive for response to 5FU and TS should be evaluated as a prognostic factor in adjuvant chemotherapy studies.
Synthetic inhibitors of Escherichia coli, calf thymus, and Ehrlich ascites tumor thymidylate synthetase.
The 5-hydroxymethyl, 5-benzyloxym methyl, and 5-azidomethyl derivatives of dUMP showed some differential inhibition; these compounds were two to three times more active against the ascites tumor enzyme than against the thymus enzyme.