Antitumor activity of novel pyridine, thiophene and thiazole derivatives

被引:0
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作者
Mostafa M. Ghorab
Mansour S. Al-Said
机构
[1] King Saud University,Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy
来源
关键词
Dihydropyridine; Thiophene; Thiazole; Antitumor activity;
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摘要
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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页码:965 / 973
页数:8
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