Browsing by Author "Gomha S.M."

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An efficient synthesis of novel pyrazole-based heterocycles as potential antitumor agents
(MDPI AG, 2017) Abdallah M.A.; Gomha S.M.; Abbas I.M.; Kazem M.S.H.; Alterary S.S.; Mabkhot Y.N.; Department of Chemistry; Faculty of Science; Cairo University; Giza; 12613; Egypt; Department of Chemistry; Faculty of Dentistry; October University for Modern Science & Arts; Giza; 12613; Egypt; Department of Chemistry; College of Science; King Saud University; P.O. Box 2455; Riyadh; 11451; Saudi Arabia
A new series of pyrazolylpyridines was prepared by reaction of ethyl-3-acetyl-1,5-diphenyl-1H-pyrazole-4-carboxylate with the appropriate aldehyde, malononitrile, or ethyl acetoacetate and an excess of ammonium acetate under reflux in acetic acid. Similarly, two novel bipyridine derivatives were prepared by the above reaction using terephthaldehyde in lieu of benzaldehyde derivatives. In addition, a series of 1,2,4-triazolo[4,3-a]pyrimidines was synthesized by a reaction of 6-(pyrazol-3-yl)pyrimidine-2-thione with a number of hydrazonoyl chlorides in dioxane and in the presence of triethylamine. The structure of the produced compounds was established by elemental analyses and spectral methods, and the mechanisms of their formation was discussed. Furthermore, the pyrazolyl-pyridine derivatives were tested as anticancer agents and the results obtained showed that some of them revealed high activity against human hepatocellular carcinoma (HEPG2) cell lines. � 2017 by the authors.
Synthesis and Antimicrobial Activity of Novel Azolopyrimidines and Pyrido-Triazolo-Pyrimidinones Incorporating Pyrazole Moiety
(HeteroCorporation, 2017) Abbas I.M.; Abdallah M.A.; Gomha S.M.; Kazem M.S.H.; Department of Chemistry; Faculty of Science; Cairo University; Giza; 12613; Egypt; Department of Chemistry; Faculty of Dentistry; October University for Modern Science and Arts University; Giza; 12613; Egypt
A new series of azolopyrimidine derivatives incorporating pyrazole moiety were synthesized by reaction of 1-(pyrazol-3-yl)-2-propenone with a number of heterocyclic amines in the presence of a catalytic amount of acetic acid. The mechanism of formation of the products was also discussed, and the structure assigned was elucidated based on both elemental and spectral analyses data. In addition, 7-(pyrazolyl)-2-thioxo-5-phenyl-1,3-dihydropyrido[2,3-d]pyrimidin-4-one was used as starting material for preparation of a new series of pyridotriazolopyrimidines via its reaction with a variety of hydrazonoyl chlorides in dioxane using triethylamines as catalyst. The assigned structure for these products was also proved via elemental analysis and spectroscopic techniques (IR, 1H NMR, and Mass). Moreover, the antimicrobial activity of some selected examples of the new products was evaluated, and the results obtained revealed high activity of compound 20a against the Gram positive bacteria Staphylococcus aureus and the Gram negative bacteria Klebsiella pneumonie. All the tested compounds have no antifungal activity. � 2017 Wiley Periodicals, Inc.
Synthesis, cytotoxicity evaluation, molecular docking and utility of novel chalcones as precursors for heterocycles incorporating pyrazole moiety
(Bentham Science Publishers B.V., 2018) Gomha S.M.; Abdallah M.A.; Abbas I.M.; Kazem M.S.H.; Department of Chemistry; Faculty of Science; Cairo University; Giza; 12613; Egypt; Department of Chemistry; Faculty of Dentistry; October University for Modern Science & Arts University; Giza; 12613; Egypt
Background: Chalcones, 2-pyrazolines and thiazoles have been reported to possess various pharmacological activities. Objective: Synthesis of new chalcones and utilizing them as a building block for constructing a series of thiazole derivatives and evaluating some of them as anticancer agents. Method: The new compounds were synthesized via stirring at room temperature or thermal heating. Cytotoxic evaluation of the new synthesized compounds was tested using the method of Skehan et al. Moreover, the computational studies were performed using MOE 2014.09 software. Result: A series of new chalcones were prepared by the reaction of ethyl 3-acetyl-1-aryl-5-methyl- 1H-pyrazole-4-carboxylate with a number of substituted benzaldehydes. One of these chalcones was used as a building block for constructing a pyrazoline ring via its reaction with thiosemicarbazide. The produced carbothioamide derivative was used for the preparation of two series of thiazole derivatives by its reaction with a number of hydrazonoyl chlorides. Moreover, reaction of 3- acetylpyrazole thiosemicarbazone derivative with a number of N-aryl-2-oxopropane hydrazonoyl chlorides afforded 5-arylazothiazole derivatives. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data. Some of the newly synthesized chalcones and thiazoles were tested for their cytotoxicity against human colon carcinoma cell line (HCT-116) and the molecular docking was carried out on the most active compound 3f. Conclusion: The results of the anticancer activity revealed that compounds 3f, 3e, 3c and 3b have promising activities compared with the standard drug Doxorubicin. Moreover, the computational studies confirm the results of biological activity. Also, the ADME profile study showed that compound 3f can be considered as a promising drug by conducting good pharmacokinetic and medicinal chemistry tests. � 2018 Bentham Science Publishers.