126931-32-6Relevant articles and documents
Condensed pyrimidine derivative
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, (2008/06/13)
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.
Pyrrolopyrimidine Folate Analogues: "Inverted" Analogues of the Cytotoxic Agent LY231514
Taylor, Edward C.,Young, Wendy B.
, p. 7947 - 7952 (2007/10/03)
N-pyrimidin-5-yl)ethyl>benzoyl>-L-glutamic acid (3a) and N-pyrimidin-5-yl)propyl>benzoyl>-L-glutamic acid (3b) were synthesized as potential anticancer agents.
Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[ω-(2-amino-4-substituted-6,7- dihydrocyclopenta[d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids
Kotake,Iijima,Yoshimatsu,Tamai,Ozawa,Koyanagi,Kitoh,Nomura
, p. 1616 - 1624 (2007/10/02)
Novel antifolates with a 6-5 fused ring system, 6,7- dihydrocyclopenta[d]pyrimidine, (3a,b and 4a,b) were synthesized on the basis of combined modification of the heterocycle and bridge regions of the folate molecule. The synthetic method involves (1) syn
A Novel Synthetic Approach to Pyrrolopyrimidine Antifolates
Miwa, Tetsuo,Hitaka, Takenori,Akimoto, Hiroshi
, p. 1696 - 1701 (2007/10/02)
A novel and efficient synthetic method for the synthesis of pyrrolopyrimidine antifolates is described.The key reaction of this method is the photo-initiated free radical addition of bromomalononitrile or ethyl bromocyanoacetate to an enol ether to afford the backbone skeleton of the targeted antifolate molecule.The key intermediates 3 or 4 are smoothly converted to the pyrrolopyrimidine antifolates 1 or 2 in three steps and in high overall yield.
Fused pyrimidines, their production and use
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, (2008/06/13)
New fused pyrimidines of the general formula (I): STR1 wherein the ring A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R1, R2, R3 and R