2-amino-6-alkyl-5-(4-substituted-1-piperazinyl) pyrimidin-4-ones

Details 2-amino-6-alkyl-5-(4-substituted-1-piperazinyl) pyrimidin-4-ones 2-amino-6-alkyl-5-(4-substituted-1-piperazinyl) pyrimidin-4-ones

1995-10-25

1997-09-23

Grumbling, Matthew V.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544295, A61K 31535, C07D40302

Patent

active

056705085

ABSTRACT:
A series of 2-amino-6-alkyl-5-(4-substituted-1-piperazinyl)pyrimidin-4-ones that have selective cytotoxicity on human CNS tumor cells.

REFERENCES:
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Dixon et al., "A Novel cDNA Restores Reduced Folate Carrier Activity and Methotrexate Sensitivity to Transport Deficient Cells", The Journal of Biological Chemistry 269:17-20, 1994.
Hodson et al., "Thienyl and Thiazolyl Acyclic Analogues of 5-Deazatetrahydrofolic Acid", J. Med. Chem. 37:2112-2115, 1994.
Kovacs et al., "Potent Antipneumocystis and Antitoxoplasma Activities of Piritrexim, a Lipid-Soluble Antifolate", Antimicrobial Agents and Chemotherapy 32:430-433, 1988.
Matherly et al., "Characterization of Transport-mediated Methotrexate Resistance in Human Tumor Cells with Antibodies to the Membrane . . . ", The Journal of Biological Chemistry 267:23253-23260, 1992.
Shih et al., "Synthesis and Biological Activity of Acyclic Analogues of 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid", J. Med. Chem 35:1109-1116, 1992.
Wang et al., "Novel Open-Ring Analogues of N.sup.5, N.sup.10 -Methylenetetrahydrofolic Acid With Selective Activity Against Brain Tumor", Bioorganic & Medicinal Chemistry Letters 5:1909-1912, 1995. Aryl)-1-Piperazinyl!-6-. . . ", Chemistry and Biology of Pteridines 69-71, 1986.

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