Abstract
Nine tripeptide analogues of methotrexate were synthesized from 2,4-diamino-6-(chloromethyl)pteridine. Only N-[N-[4-[2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]glycyl-DL-aspartic acid (1a) showed moderate activity against L1210 murine leukemia (ILS = 69%) and W 256 carcinosarcoma (TGI = 55%).
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