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Quinoline antifolate thymidylate synthase inhibitors: variation of the C2-and C4-substituents

…, N Roberts, JAM Bishop, BM O'Connor…

文献索引:Warner; Barker; Jackman; Burrows; Roberts; Bishop; O'Connor; Hughes Journal of Medicinal Chemistry, 1992 , vol. 35, # 15 p. 2761 - 2768

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被引用次数: 18

摘要

3, 4dihydro-4-oxo-6-quin~~ yl) methyl]-N-prop2-yny~ ino] benzoyl]-~-glutamic acid (1, CB3717) have led to the synthesis of a series of quinoline antifolates bearing a variety of substituents at the C2 and C4 positions. In general the synthetic route involved the coupling of the appropriate diethyl N-[4-(prop2-ynylamino) benzoyl]-~-glutamate with a disubstituted 6- (bromomethy1) quinoline followed by deprotection using mild alkali. The compounds were ...