title: Antitumor activity of novel pyridine, thiophene and thiazole derivatives.
abstract: 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, (1)H-NMR, (13)C-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 IC(50) values (54.54, 61.57 μM), 8 when compared with a reference drug IC(50) value (68.99 μM), while compound 5 is nearly as active as doxorubicin (CAS 23214-92-8).
authors.affiliation: Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. mmsghorab@yahoo.com
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.forename: Mansour S
authors.initials: MS
authors.lastname: Al-Said
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor / Q000473:pathology*; D016923:Cell Death / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000494:pharmacology; D005260:Female; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011725:Pyridines; D013844:Thiazoles; D013876:Thiophenes; D004317:Doxorubicin