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Syntheses and antifolate activity of 5-methyl-5-deaza analogues of aminopterin, methotrexate, folic acid, and N10-methylfolic acid.
TLDR
Investigation of 5-methyl-5-deaza analogues for their effect on cell growth inhibition, transport characteristics, and net accumulation of polyglutamate forms revealed the analogues to have essentially the same properties as the appropriate parent compound, aminopterin or methotrexate (MTX), except that 20 and 21 were approximately 10 times more growth inhibitory than MTX.
Quantitation of folic acid enhancement of antifolate synergism.
TLDR
The dramatic intensity of the synergism between DDATHF and TMTX at 40 microM PteGlu, along with the concept of modulation of antifolate synergism by folates, suggests future in vivo and/or clinical applications of combinations of these (or similar) compounds.
10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism.
TLDR
The in vivo results vs. L1210 leukemia and S180 ascites offered evidence that 8c might have a better therapeutic index against this tumor than methotrexate, but no other result from either of these compounds suggested significant superiority over metHotrexate.
Identification of a novel dimeric phosphoprotein (PP29/30) associated with signaling receptors in human T lymphocytes and natural killer cells
Two-dimensional gel electrophoresis of in vitro phosphorylated proteins coprecipitated by CD2 monoclonal antibody (mAb) from Brij58 lysates of resting human T lymphocytes and natural killer (NK)
Polyglutamyl derivatives of tetrahydrofolate as substrates for Lactobacillus casei thymidylate synthase.
TLDR
Tetrahydropteroylpolyglutamates containing up to seven Glu residues were tested as substrates for Lactobacillus casei thymidylate synthase; however, with the phosphonate derivative of fluorodeoxyuridine, the polyglutamate substrate enhanced inhibition 5- to 8-fold.
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