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• W2083583820 abstract "Thirteen novel benzazole derivatives were synthesized as possible anticancer agents. The first intermediate 1,3-benzothiazol-2-ylacetonitrile (2) was synthesized via cyclodeamination reaction of o-aminothiophenol (1) with malononitrile. Also, the second intermediate 5,6-dimethyl-1H-benzimidazol-2-ylacetonitrile (10) was afforded via cyclocondensation reaction between 4,5-dimethyl-1,2-phenylenediamine (9) and ethylcyanoacetate. Nucleophilic reaction of benzimidazolyl NH of compound (10) with ethylcyanoacetate afforded benzimidazolyl-3-oxopropanenitrile (11). On the other hand, methylenation of CH2 function of compound (10) with dimethylformamide/dimethylacetal afforded benzimidazolylprop-2-enenitrile 12. The synthesis of benzothiazoylpyridines 5a,b and 8a,b as well as benzimidazolylpyridines, 14a,b and 17a–d was carried out through Michael addition of compounds 2 or 10 with arylidenemalononitriles 3a,b and 4a–d. The combination of pharmacophoric anticancer moieties, pyridine and benzazoles was the base on which target compounds 5a,b, 8a,b, 14a,b and 17a–d were designed. Among the synthesized compounds, four derivatives 10 and 17b–d were selected by National Cancer Institute (NCI), USA to be screened for their anticancer activity at a single high dose (10−5 M) against a panel of 60 cancer cell lines. Compound 17b 4-[p-chlorophenyl]pyridine and 17d 4-[p- methoxyphenyl] pyridine exhibited a broad and moderate antitumor activity against 41 tumor cell lines belonging to the nine subpanels employed and are selected for further evaluation at five dose level screening." @default.
• W2083583820 created "2016-06-24" @default.
• W2083583820 creator A5040308530 @default.
• W2083583820 date "2011-09-01" @default.
• W2083583820 modified "2023-10-16" @default.
• W2083583820 title "Synthesis, characterization of some benzazoles bearing pyridine moiety: Search for novel anticancer agents" @default.
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• W2083583820 doi "https://doi.org/10.1016/j.ejmech.2011.05.075" @default.
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