5-Fluoropyrimidin-2-one, a new metaphase arresting agent.

  title={5-Fluoropyrimidin-2-one, a new metaphase arresting agent.},
  author={R. Oftebro and O. Grimmer and T. B. Oyen and S. Laland},
  journal={Biochemical pharmacology},
  volume={21 18},
Abstract 5-Fluoropyrimidin-2-one arrests reversibly the Chang strain of human liver cells in the metaphase. The effect is dependent on the presence of the halogen in the molecule and seems to be due to the substance per se. 
A new purine analogue with antimitotic activity.
The compound 4-benzylamino 6-methyl 7-benzyl pyrrolo [2,3-d] pyrimidine has been found to arrest cultured cells in metaphase and some irreversible effects occur, such as anarchic reconstruction of the nuclear membrane around dispersed chromosomes and formation of multinucleated giant cells. Expand
Metahalones, a new class of metaphase inhibitors
The results suggest that the metaphase-inhibitory activity is associated with the 2-0~0 group and the 5-halogen, and that certain substituents in other positions are permissable for the retainment of activity. Expand
Interaction of 1-propargyl-5-chloropyrimidin-2-one (a metahalone) with rat brain tubulin.
The binding of 1-propargyl-5-chloropyrimidin-2-one to tubulin at or near the colchicine binding site may be responsible for the metaphase arresting characteristics of this drug. Expand
Structure-activity relationship of 1-propargyl-5-halopyrimidin-2-ones
SummaryThe structure-activity relationship of 1-propargyl-5-halopyrimidin-2-ones with respect to mitotic inhibitory potential and inhibition of colchicine binding to tubulin was investigated. AExpand
Inhibitory effects of the new mitotic inhibitor 5-chloropyrimidin-2-one and of vincristine on human cells in vitro.
The results reveal that the metaphase-arresting agents NY 3000 and vincristine act also in the interphases of proliferating cells, however, the mechanism behind the interphase effect seems to be different for the two drugs. Expand
Effects of the new mitotic inhibitor pyrimidinsulfone NY 4137 on human cells in vitro and on colchicine binding to tubulin
The binding of NY 4137 to tubulin at or near the colchicine binding site may be responsible for the metaphase arrest. Expand
Mitotic arrest and interphase inhibition induced by the pyrimidine sulfoxide NY 4138
The metaphase arrest induced by the sulfoxide 5-bromo-2-(2-thienylmethyl)sulfinyl-pyrimidine (NY 4138) was studied on synchronized human NHIK 3025 cells cultivated in vitro and was characterized as irreversible. Expand
Pyrimidinones as biodynamic agents.
  • A. K. Saxena, S. Sinha
  • Chemistry, Medicine
  • Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques
  • 1987
The pyrimidinone moiety may be considered as an important pharmacophore for incorporation in the design of molecules of biological interest in view of the diverse types of biological activities associated with p Skyrimidinones and molecules having pyrimidine as a component substructure. Expand
Resistance to the mitotic inhibitor NY 3170 in Chinese hamster ovary cells.
This work has isolated CHO cells which are resistant to NY 3170, a member of the metahalone group of antimitotic drugs, and found that other mutants, selected on the basis of vincristine resistance, are cross-resistant to New York 3170. Expand
Cell-cycle inhibitory effects of the mitotic inhibitor NY 3170 on human cells in vitro.
It was shown that the presence of NY 3170 during mitosis is a necessary and sufficient condition for metaphase Arrest, thus demonstrating that metaphase arrest is not dependent on some preceding event in interphase. Expand


Synthesis and properties of ribosylpyrimidin-2-one.
When growing Escherichia coli K-12 in the presence of ribosylpyrimidin-2-one, an unbalanced growth and cell elongation resulted and the syntheses of RNA and of protein were not affected, while the synthesis of DNA was strongly inhibited. Expand
Synthesis of pyrimidin-2-one deoxyribosides and their ability to support the growth of the deoxyriboside-requiring organism Lactobacillus acidophilus R 26.
The attention was drawn to a substance which exhibited a violet fluorescence when exposed to ultraviolet light, which had a maximnum light absorption in OlNhydrochloric acid at 324 m,i and no absorption at 260 m,u, and which supported the growth of the deoxyriboside-requiring strain Lactobacillu8 acidophilu8 R26 Orla Jensen. Expand
The Presence in Mammalian Liver and Blood of Substances which Inhibit the Mitotic Activity of Human Cells Grown in Vitro
The Presence in Mammalian Liver and Blood of Substances which Inhibit the Mitotic Activity of Human Cells Grown in vitro
It is concluded that a true genetic difference exists in these cell lines, from dispersed single cells obtained by trypsinization of a specimen of human embryonic lung, from which both fibroblastic and epithelioid cells have been obtained. Expand
5-fluoropyrimidin-2-one deoxyriboside and its growth-inhibiting properties.
Some Derivatives of 5-Fluoropyrimidine.