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10-Ethyl-10-deaza-aminopterin: structural design and biochemical, pharmacologic, and antitumor properties.
The new folate analog 10-ethyl-10-deaza-aminopterin (10EdAM) was equivalent to methotrexate (MTX) as an inhibitor of dihydrofolate reductase, but was more effectively transported and polyglutamylatedExpand
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Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
Successive alkylation of dimethyl homoterephthalate with propargyl bromide and 2,4-diamino-6-(bromomethyl)pteridine followed by ester saponification at room temperature affordedExpand
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New folate analogs of the 10-deaza-aminopterin series: markedly increased antitumor activity of the 10-ethyl analog compared to the parent compound and methotrexate against some human tumor
In an extension of our prior studies in murine tumor models, we examined two new folate analogs in the 10-deaza-aminopterin series for antitumor activity against a group of human tumor xenografts inExpand
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Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
Requirements for large-scale synthesis of the potent antitumor drug 10-deazaminopterin have led to development of a facile synthesis of this compound and its 10-alkyl analogues. The lithiumExpand
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Potential histidine decarboxylase inhibitors. 1. alpha- and beta-substituted histidine analogues.
Histidine analogues with alkyl substitution at Calpha and Cbeta were prepared as potential inhibitors of specific histidine decarboxylase. Activity was assessed in vitro using extracts of rat pyloricExpand
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