Quinazoline antifolate thymidylate synthase inhibitors: Replacement of glutamic acid in the C2-methyl series
The synthesis of a series of analogues of the potent thymidylate synthase (TS) inhibitor N-[4[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N- prop-2-ynylamino]benzoyl]-L-glutamic acid (ICI 198583, 1) is described in which the glutamic acid residu
The Synthesis and Thymidylate Synthase Inhibitory Activity of L-γ-L-Linked Dipeptide and L-γ-Amide Analogues of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic Acid (ICI 198583)
Sixteen γ-linked dipeptide and four L-Glu-γ-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) have beensynthesized and evaluated as inhibitors of thymidylate synthase (TS).Z-blocked L-Glu-γ-L-linked dipepti
Bisset, Graham M. F.,Bavetsias, Vassilios,Thornton, Timothy J.,Pawelczak, Krzysztof,Calvert, A. Hilary,et al.
p. 3294 - 3302
(2007/10/02)
Syntheses and Thymidylate Synthase Inhibitory Activity of the Poly-γ-glutamyl Conjugates of N--2-thenoyl>-L-glutamic Acid (ICI D1694) and Other Quinazoline Antifolates
Thirteen poly-γ-glutamates derived from several novel antifolates have been synthesized by a convergent route.The syntheses of poly-γ-glutamyl conjugates of N--2-thenoyl>-L-glutamic aci
Bisset, Graham M. F.,Pawelczak, Krzysztof,Jackman, Ann L.,Calvert, A. Hilary,Hughes, Leslie R.
p. 859 - 866
(2007/10/02)
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