Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series

…, R Kimbell, BM O'Connor, AH Calvert…

文献索引：Marsham; Jackman; Barker; Boyle; Pegg; Wardleworth; Kimbell; O'Connor; Calvert; Hughes Journal of Medicinal Chemistry, 1995 , vol. 38, # 6 p. 994 - 1004

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被引用次数: 36

摘要

[N-[(3, 4-dihydro-2-methyl-4-oxo-6-quinazolinyl~ methy11-N-prop-2-yny1amino1benzoy11- ~-g1utam-ic acid (IC1 198583, 1) is described in which the glutamic acid residue has been replaced by other a-amino acids. Most of these analogues were prepared by coupling of tert- butyl-4-(prop-2-yny1amino) benzoate (37) with 6-(bromomethyl)-3, 4-dihydro-2-methyl-4- oxoquinazoline (34) followed by deprotection of the tert-butyl ester to the acid and azide- ...