157701-51-4Relevant academic research and scientific papers
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors
Marsham, Peter R.,Wardleworth, J. Michael,Boyle, F. Thomas,Hennequin, Laurent F.,Kimbell, Rosemary,Brown, Melody,Jackman, Ann L.
, p. 3809 - 3820 (2007/10/03)
The synthesis is described of a series of analogues of the potent thymidylate synthase (TS) inhibitor, N-[4-[N-[(3,4-dihydr0-2,7-dimethyl-4- oxo-6-quinazolinyl)methyl]-N-prop-2-ynylamino]2-fluorobenzoyl]-L-glutamic acid (4, ZM214888), in which the glutami
Tricyclic compounds with pharmaceutical activity
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, (2008/06/13)
The invention relates to tricyclic compounds of formula (I) STR1 wherein R1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R3 includes a group of the formula --NHCH(CO2 H)--A1 --Y1 wherein A1 is (1-6C)alkylene and Y1 is carboxy, tetrazol-5-yl, N-?(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.
