Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogs in the C2-methyl series

PR Marsham, AL Jackman, AJ Hayter…

文献索引：Marsham, Peter R.; Jackman, Ann L.; Hayter, Anthony J.; Daw, Melanie R.; Snowden, Jayne L.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2209 - 2218

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被引用次数: 12

摘要

Several C2-methylquinazoline-based antifolates (14-26) have been prepared in which the C9, NlO bridge has been replaced by the reversed N9, ClO unit. This series was extensively studied by incorporating further substituents at N9 and C10 as well as by modifications to the p-aminobenzoate ring. The C2-methylquinazoline analogues 29, 30, and 31 containing the methyleneoxa, methylenethia, and thia bridge units were also synthesized. In general ...