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KMID : 0043319960190010062
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Archives of Pharmacal Research
1996 Volume.19 No. 1 p.62 ~ p.65
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Synthesis and in vitro cytotoxicity of a homologous series of 5-halosubstituted 1,3-Bis(ω-cyanoalkyl)uracil analogues
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Kim Jack-C.
Dong Eun-Soo
Park Jin-Il
Kim Young-Hyun
Choi Soon-Kyu
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Abstract
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A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations ranged from 2.2 to ). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.
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KEYWORD
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Acyclic Nucleoside, Antitumor Activity, Mouse mam-mary carcinoma (FM-3A), Mouse lymphoid neoplasma (P-388), Human histiocytic lymphoma (U-937), Inhibitory concentration
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