Tosylproline analogs as thymidylate synthase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514 75, 514 91, 514142, 514359, 514381, 514382, 514425, 514428, 514538, 514541, 514542, 514603, 514608, 514617, 514620, 514646, 514784, 548253, 548254, 548255, 548542, 548547, 560429, 560430, 560433, 560442, 562 11, 562 14, 562 15, 562 16, 562 30, 562 44, 564163, A61K 31401, A61P 3100, A61P 3500, C07D20748

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active

06143776&

ABSTRACT:
Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

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Jackman et al., "The Antitumour Activity of ZD9331, a Non-polyglutamatable Quinazoline Thymidylate Synthase Inhibitor", pp. 185-188 in Purine and Pyrimidine Metabolism in Man VIII, ed. Sahota and Taylor, Plenum Press, New York (1995).
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