A potent multisubstrate analog inhibitor of human thymidylate synthetase

…, V Amarnath, AD Broom, FC Fou…

Index: Srinivasan, Ananthachari; Amarnath, Venkataraman; Broom, Arthur D.; Zou, F. C.; Cheng, Yung-Chi Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1710 - 1717

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Citation Number: 20

Abstract

Alkylation of diethyl 5, 6, 7, 8-tetrahydro-8-deazafolate with 3'-0-acetyl-5-(bromomethyl)-2'- deoxyuridine 5'-[bis-(trichlorethyl) phosphate], followed by removal of the trichloroethyl groups with a Zn/Cu couple and mild saponification, gave the target inhibitor N-[4-[[[2-amin0- 3, 4, 5, 6, 7, 8-hexahydro-4-0~ 0-5-[(2'-deoxyuridin-5-yl) methyl]-pyrido [3, 2-d] pyrimidin-6-yl] methyl] amino] benzoyl]-~-glutamic acid 5'-monophosphate. The free nucleoside and the 5 ...

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