Synthesis and biological activity of open-chain analogs of 5, 6, 7, 8-tetrahydrofolic acid-potential antitumor agents

…, D Wilson, DS Duch, GK Smith, R Ferone

Index: Bigham; Hodson; Mallory; Wilson; Duch; Smith; Ferone Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1399 - 1410

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Citation Number: 33

Abstract

DACTHF). Benzene ring substituted analogues were synthesized from a protected pyrimidinyl propionaldehyde and a substituted benzoyl glutamate moiety by a key reductive amination step. Pyrimidine and linking chain subetituted analogues were built up stepwise from p-aminobenzoic acid or analogues. The compounds were teated as inhibitors of methotrexate uptake as a measure of binding to the reduced folate tramport system, as ...