- Pyrrolo[2,3-d]pyrimidine thymidylate synthase inhibitors: Design and synthesis of one-carbon bridge derivatives
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A series of novel pyrrolo[2,3-d]pyrimidine derivatives was designed and synthesized as thymidylate synthase (TS) inhibitors. Molecular design was performed on the human TS complex model built on the basis of the reported structure of TS-deoxyuridinemonoph
- Aso,Imai,Yukishige,Ootsu,Akimoto
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p. 1280 - 1287
(2007/10/03)
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- Condensed pyrimidine derivative
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A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: STR1 wherein R1 represents a hydroxyl or amino group; R2 represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, --CO2 R5 and --CO2 R6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part STR2 A represents an oxygen atom, a group represented by the formula: STR3 (wherein R3 and R4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R3 and R4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: STR4 (wherein R70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.
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- Novel 6-5 fused ring heterocycle antifolates with potent antitumor activity: Bridge modifications and heterocyclic benzoyl isosters of 2,4-diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine antifolate
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Structural modifications of an extremely potent inhibitor of dihydrofolate reductase (DHFR) activity and tumor cell growth, N-[4-[3-(2,4-diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidin-5-yl)propyl ]benzoyl]-L-glutamic acid (1), have led to the synthesis of
- Kotake,Okauchi,Iijima,Yoshimatsu,Nomura
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p. 829 - 841
(2007/10/02)
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