Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / therapeutic use
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Glutamates / chemical synthesis*
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Glutamates / chemistry
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Glutamates / therapeutic use
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Guanine / analogs & derivatives*
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Guanine / chemical synthesis
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Guanine / therapeutic use
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Humans
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Leukemia L1210 / drug therapy
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Leukemia, Lymphoid / drug therapy
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Mice
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Pemetrexed
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Structure-Activity Relationship
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Thymidylate Synthase / antagonists & inhibitors*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Glutamates
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Pemetrexed
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Guanine
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Thymidylate Synthase