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KMID : 0043320120350060965
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Archives of Pharmacal Research
2012 Volume.35 No. 6 p.965 ~ p.973
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Antitumor activity of novel pyridine, thiophene and thiazole derivatives
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Ghorab Mostafa M.
Al Said Mansour S.
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Abstract
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2-Cyano-N’-[1-(2,5-dimethoxyphenyl)]ethylideneacetohydrazide 1 was obtained via reaction of cyanoacetic acid hydrazide with 2,5-dimethoxyacetophenone. A number of novel pyridines 2a?j, 3, 4, thiophenes 5?9 and thiazoles 10?12 were prepared by using the hydrazide-hydrazone derivative 1 as a starting material. The structure of the newly synthesized compounds was characterized by elemental analyses, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro antitumor activity against Ehrlich Ascites Carcinoma (EAC) cells. Compounds 2j and 6 showed a higher activity with IC50 values (54.54, 61.57 μM), 8 when compared with a reference drug IC50 value (68.99 μM), while compound 5 is nearly as active as Doxorubicin (CAS 23214-92-8).
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KEYWORD
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Dihydropyridine, Thiophene, Thiazole, Antitumor activity
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