A DIDEAZATETRAHYDROFOLATE ANALOG LACKING A CHIRAL CENTER AT C-6, N-[4-[2-(2-AMINO-3,4-DIHYDRO-4-OXO-7H-PYRROLO[2,3-D]PYRIMIDIN-5-YL)ETHYL]BENZOYL]-L-GLUTAMIC ACID, IS AN INHIBITOR OF THYMIDYLATE SYNTHASE
A DIDEAZATETRAHYDROFOLATE ANALOG LACKING A CHIRAL CENTER AT C-6, N-[4-[2-(2-AMINO-3,4-DIHYDRO-4-OXO-7H-PYRROLO[2,3-D]PYRIMIDIN-5-YL)ETHYL]BENZOYL]-L-GLUTAMIC ACID, IS AN INHIBITOR OF THYMIDYLATE SYNTHASE
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DOI：
10.1021/jm00101a023
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发表时间：
1992-11-13
影响因子：
7.3
通讯作者：
MORAN, RG
中科院分区：
文献类型：
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作者：
TAYLOR, EC;KUHNT, D;MORAN, RG
N-[4-[2-(2-氨基-3,4-二氢-4-氧代-7H-吡咯并[2,3-d]嘧啶-5-基)乙基]苯甲酰基]-L-谷氨酸 (15) 由 2-新戊酰基-7-脱氮鸟嘌呤经过五个步骤制备而成，已被发现是一种抗肿瘤剂，其主要作用位点是胸苷酸合酶而不是嘌呤合成。该化合物似乎是临床评估的有希望的候选者。
N-[4-[2-(2-Amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid (15), prepared in five steps from 2-pivaloyl-7-deazaguanine, has been found to be an antitumor agent with its primary site of action at thymidylate synthase rather than purine synthesis. This compound appears to be a promising candidate for clinical evaluation.