Abstract
A new series of pyrazole, bipyridine, N-amide derivatives and Schiff bases was synthesized using compound 2-(3-cyano-6- (thiophen-2-yl)-4,4′- bipyridin-2-yloxy) acetohydrazide (3) as a starting material. The compounds structures were confirmed depending on the spectroscopic methods and elemental analysis. Also, the compounds were evaluated as anticancer agents by the compounds screened towards adenocarcinoma breast cancer cell line (MCF-7). The compounds showed a promising cytotoxic effect against human breast cancer cells. Compound 7c showed the most effective activity compared to other compounds with (IC50 = 0.6 ± 0.01 μg mL−1) in comparison with the reference drug doxorubicin (IC50 = 1.6 ± 0.02 μg mL−1). While compound 3 is closely active with doxorubicin. Also compounds 2, 4, 6, 7a, 7b and 7d showed noticeable cytotoxic effect. Early and late apoptotic cells were detected using Acridine orange/Ethidium bromide staining technique. The results of biologically screening of the tested compounds give an idea about the importance in the compounds acting against breast cancer and may lead to the discovery of a potent anticancer agent.
Highlights
Cancer disease is one of the most widely spread diseases nowadays especially breast cancer
Chemistry In this research, a one-pot manner was used for the synthesis of compound2-oxo-4-(pyridin-4-yl)-6-(thiophen2-yl)-1,2-dihydropyridine-3-carbonitrile (1) where all the reaction components, 2-acetylthiophene, 4-pyridine carboxaldehyde, ammonium acetate, and ethyl cyanoacetate were added in the presence of ceric ammonium nitrate (CAN) and refluxed in ethanol
All other signals appeared at their expected position as illustrated in the experimental section. 2-(3-Cyano-6-(thiophen-2-yl)-4,4′bipyridin-2-yloxy)acetohydrazide (3), is used as a starting matter for the synthesis of all target compounds in this work (Scheme 1)
Summary
Cancer disease is one of the most widely spread diseases nowadays especially breast cancer. Breast cancer comes in various forms either histological or clinical because it is a heterogeneous disease. Its treatment is done through chemotherapy and/or hormone therapy. Heterocyclic compounds that incorporating pyridine moiety appear miscellaneous pharmacological properties such as anticancer [1], antimicrobial [2, 3], anticonvulsant [4], antiviral [5], anti- HIV [6], antifungal and, antibacterial activities [7]. The antitumor activity of pyridine ring enhanced by introducing different substituents such as. Al Shareef B MC Chemistry (2020) 14:40 and studying their antitumor activity against breast cancer cell line
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