Abstract
1-(2,4-Dichlorophenyl)-3-(4-fluorophenyl)propen-1-one (1) was prepared and reacted with an active methylene compound (ethyl cyanoacetate) in the presence of ammonium acetate to give the corresponding cyanopyridone 2. Compound 2 reacted with hydrazine hydrate, malononitrile, ethyl bromoacetate and phosphorous oxychloride to afford compounds 4 and 7–11, respectively. The 2-chloropyridine derivative 11 reacted with different primary amines, namely benzyl amine, piperonyl amine, 1-phenylethyl amine, and/or the secondary amines 2-methyl-pipridine and morpholine to give the corresponding derivatives 12–15. Hydrazinolysis of chloropyridine derivative 11 with hydrazine hydrate afforded the corresponding hydrazino derivative 17. Condensation of compound 17 with ethyl acetoacetate, acetylacetone, isatin and different aldehydes gave the corresponding derivatives 18–21. Some of newly synthesized compounds were screened for cytotoxic activity against three tumor cell lines. The results indicated that compounds 8 and 16 showed the best results, exhibiting the highest inhibitory effects towards the three tumor cell lines, which were higher than that of the reference doxorubicin and these compounds were non-cytotoxic towards normal cells (IC50 values > 100 μg/mL).
Highlights
Cancer is the second leading cause of death in both developing and developed countries [1]
The synthesis of the designed target compounds was achieved as outlined in Schemes 1–3
The synthesisthe of pyridin-3-carbonitrile the designed target compounds was 2achieved as outlined in Schemesof1–3
Summary
Cancer is the second leading cause of death in both developing and developed countries [1]. Despite the fact that there is a large amount of information available dealing with the clinical aspects of cancer chemotherapy, we felt that there was a clear requirement for an updated treatment from the point of view of medicinal chemistry and drug design [6]. Another major goal for developing new anticancer agents is to overcome cancer resistance to drug treatment, which has made many of the currently available chemotherapeutic agents ineffective [7].
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