Synthesis, Antitumor Evaluation and Molecular Docking of New Morpholine Based Heterocycles
AbstractA series of new morpholinylchalcones was prepared and then used as building blocks for constructing a series of 7-morpholino-2-thioxo-2,3-dihydropyrido[2,3-d]pyrimidin-4(1H)-ones via their reaction with 6-aminothiouracil. The latter thiones reacted with the appropriate hydrazonoyl chloride to give the corresponding pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5(1H)-ones. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data and the mechanisms of their formation were also discussed. Most of the synthesized compounds were tested for in vitro activity against human lung cancer (A-549) and human hepatocellular carcinoma (HepG-2) cell lines compared with the employed standard antitumor drug (cisplatin) and the results revealed that compounds 8, 4e and 7b have promising activities against the A-549 cell line (IC50 values of 2.78 ± 0.86 μg/mL, 5.37 ± 0.95 μg/mL and 5.70 ± 0.91 μg/mL, respectively) while compound 7b has promising activity against the HepG-2 cell lines (IC50 = 3.54 ± 1.11 μg/mL). Moreover, computational studies using MOE 2014.09 software supported the biological activity results. View Full-Text
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Muhammad, Z.A.; Edrees, M.M.; Faty, R.A.M.; Gomha, S.M.; Alterary, S.S.; Mabkhot, Y.N. Synthesis, Antitumor Evaluation and Molecular Docking of New Morpholine Based Heterocycles. Molecules 2017, 22, 1211.
Muhammad ZA, Edrees MM, Faty RAM, Gomha SM, Alterary SS, Mabkhot YN. Synthesis, Antitumor Evaluation and Molecular Docking of New Morpholine Based Heterocycles. Molecules. 2017; 22(7):1211.Chicago/Turabian Style
Muhammad, Zeinab A.; Edrees, Mastoura M.; Faty, Rasha A.M.; Gomha, Sobhi M.; Alterary, Seham S.; Mabkhot, Yahia N. 2017. "Synthesis, Antitumor Evaluation and Molecular Docking of New Morpholine Based Heterocycles." Molecules 22, no. 7: 1211.
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