Phase I and Pharmacokinetic Study of 10-Propargyl-10-deazaaminopterin , a New Antifolate 1

Abstract

The 10-deazaaminopterins are a new class of rationally designed antifolates demonstrating greater antitumor effects than methotrexate in murine tumor models and human tumor xenografts. Their design was aimed at improving membrane transport and polyglutamylation in tumor cells, resulting in increased intracellular accumulation and enhanced cytotoxicity… (More)

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