潜在的抗癌剂。17. 带有三肽侧链的甲氨蝶呤类似物。
Potential anticancer agents. 17. Analogues of methotrexate with a tripeptide side chain.
作者信息
Suster D C, Tărnăuceanu E, Botez G, Dobre V, Niculescu-Duvăz I
出版信息
J Med Chem. 1978 Nov;21(11):1165-7. doi: 10.1021/jm00209a016.
PMID:722723
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%).
摘要
以2,4-二氨基-6-(氯甲基)蝶啶为原料合成了9种甲氨蝶呤的三肽类似物。只有N-[N-[4-[2,4-二氨基-6-蝶啶基)甲基]氨基]苯甲酰基]甘氨酰-DL-天冬氨酸(1a)对L1210小鼠白血病(ILS = 69%)和W 256癌肉瘤(TGI = 55%)表现出中等活性。
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