- SYNTHESIS OF CYCLOPENTAQUINAZOLINES
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A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-{N-{4- [N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin
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Page/Page column 61-62
(2012/02/05)
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- Quinazoline thymidylate synthase inhibitors
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The invention relates to quinazoline derivatives or pharceutically-acceptable salts thereof, which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 is (1-4C)alkyl; the quinazoline ring may optionally bear one or two further substituents selected from halogeno, (1-4C)alkyl and (1-4C)alkoxy; R2 is hydrogen or (1-4C)alkyl; R3 includes hydrogen and (1-4C)alkyl; and Ar is optionally substituted phenylene or heterocyclene; or a pharmaceutically-acceptable salt or ester thereof.
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- Quinazoline antifolate thymidylate synthase inhibitors: Replacement of glutamic acid in the C2-methyl series
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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
- Marsham,Jackman,Barker,Boyle,Pegg,Wardleworth,Kimbell,O'Connor,Calvert,Hughes
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p. 994 - 1004
(2007/10/02)
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- 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
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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.
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p. 859 - 866
(2007/10/02)
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