- New Anticancer Agents: Chiral Isomers of Ethyl 5-Amino-1,2-dihydro-2-methyl-3-phenylpyridopyrazine-7-carbamate
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Racemic ethyl 5-amino-1,2-dihydro-2-methyl-3-phenylpyridopyrazine-7-carbamate (1a) has shown antitumor activity in a variety of in vivo experiments.The preparation of the R (9) and S (10) isomers gave compounds with significant differences in potency in several biological tests.
- Temple, Carroll,Rener, Gregory
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p. 2089 - 2092
(2007/10/02)
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- '(2S)-(5-amino-1,2-dihydro-2-methyl-3-phenylpyrido(3,4-b)pyrazin-7-yl)-carbamic acid, ethyl ester
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The (2S)-(-)-isomer of (5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazin-7-yl)arbamic acid, ethyl ester is significantly more potent than either the (2R)-(+)-isomer or the (R,S)-(±)- racemic mixture in inhibiting mitotic cell division of L1210 leukemia cells. The compound, pharmaceutical compositions containing the compound, and a method of ameliorating cancer diseases in mammals are disclosed.
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