Potential anticancer agents. 17. Analogues of methotrexate with a tripeptide side chain.
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%).
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D007939:Leukemia L1210 / Q000188:drug therapy; D008727:Methotrexate / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D051381:Rats; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D008727:Methotrexate