Browsing by Author "Mahmoud A.E."

Now showing 1 - 2 of 2

Novel synthesis and antitumor evaluation of polyfunctionally substituted heterocyclic compounds derived from 2-cyano-N-(3-cyano-4,5,6,7- tetrahydrobenzo[b]thiophen-2-yl)-acetamide
(2011) Shams H.Z.; Mohareb R.M.; Helal M.H.; Mahmoud A.E.; Department of Chemistry; Faculty of Science; Helwan University; Ain Helwan; Cairo; Egypt; Department of Organic Chemistry; Faculty of Pharmacy; October University for Modern Sciences and Arts; October City; Egypt; Department of Chemistry; Faculty of Science; Cairo University; Giza; Egypt
The reaction of 2-amino-3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophene with ethyl cyanoacetate gave 2-cyano-N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2- yl)-acetamide. The latter was used to synthesize different heterocyclic derivatives comprising thiophene, thiazole, pyrazole, pyridine, pyrimidine, and coumarin rings. The mechanistic and synthetic pathways depended on regioselective attack and/or cyclization by the cyanoacetamido moiety in the key precursor on various chemical reagents. The competition of the reaction pathways including dipolar cyclization, dinucleophilic-bielectrophilic attack, ?-attack, Gewald-type attack, and condensation reactions led to the diversity of the synthesized products. The antitumor activities of the synthesized products were studied and evaluated. Most of the compounds revealed high inhibitory effects when screened in vitro for their antiproliferative activity. Three human cancer cell lines, namely, breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) were used in the screening tests. The simplicity of the synthetic procedures which mainly involved one-pot reactions under mild reaction conditions, the convenience of yield production and the diversity of the reactive sites in the produced systems play a valuable role for further heterocyclic transformations and further biological investigations. � 2010 by the authors.
Synthesis and cytotoxic activity of certain benzothiazole derivatives against human MCF-7 cancer cell line
(Blackwell Publishing Ltd, 2017) Mohamed L.W.; Taher A.T.; Rady G.S.; Ali M.M.; Mahmoud A.E.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA) University; Cairo; Egypt; Directorate of Health Affairs; Ministry of Health; Giza; Egypt; Biochemistry Department; Division of Genetic Engineering and Biotechnology; National Research Centre; Giza; Egypt
A new series of benzothiazole has been synthesized as cytotoxic agents. The new derivatives were tested for their cytotoxic activity toward the human breast cancer MCF-7 cell line against cisplatin as the reference drug. Many derivatives revealed good cytotoxic effect, whereas four of them, 4, 5c, 5d, and 6b, were more potent than cisplatin, with IC50 values being 8.64, 7.39, 7.56, and 5.15�?m compared to 13.33�?m of cisplatin. The four derivatives� cytotoxic activity was accompanied by regulating free radicals production, by increasing the activity of superoxide dismutase and depletion of intracellular reduced glutathione, catalase, and glutathione peroxidase activities, accordingly, the high production of hydrogen peroxide, nitric oxide, and other free radicals causing tumor cell death as monitored by reduction in the synthesis of protein and nucleic acids. Most of the tested compounds showed potent to moderate growth inhibitory activity; in particular, compound 6b exhibited the highest activity suggesting it is a lead compound in cytotoxic activity. � 2016 John Wiley & Sons A/S.