Browsing by Author "Taher A.T."

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Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds
(Elsevier Masson SAS, 2017) El-Meligie S.; Taher A.T.; Kamal A.M.; Youssef A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; 11561; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy and Drug Manufacturing; Misr University for Science and Technology; Giza; Egypt
A series of chalcone analogous compounds were designed and synthesized. Replacing/substituting the enone or ethylenic bridge of the parent chalcone with rigid heterocyclic moieties or substituted aromatic amines gave nineteen target compounds. Their cytotoxic activities were screened against both breast and liver cancer cells as well as breast and liver normal cells. Target compounds were also evaluated for their inhibition activity of tubulin beta polymerization. Target compound 2e, 3a, 3b, 3c, 4a-4d, 5a, 5b and 6 showed broad spectrum excellent anticancer activity against both MCF-7 and HepG2. Compound 4a showed the most TUBb inhibition activity. � 2016 Elsevier Masson SAS
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.
Synthesis and cytotoxic activity of certain trisubstituted azetidin-2-one derivatives as a cis-restricted combretastatin A-4 analogues
(Pharmaceutical Society of Korea, 2017) Elmeligie S.; Taher A.T.; Khalil N.A.; El-said A.H.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); 6th October City; Giza; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Misr University for Science and Technology; 6th October City; Giza; Egypt
Novel series of 1,3,4-trisubstituted azetidin-2-one derivatives 8a�p were synthesized and proposed as cytotoxic agents acting via inhibition of tubulin at the colchicine binding site. The design of the target compounds was based upon modification in the structure of the vascular targeting agent combretastatin A-4 (CA-4). The cis double bond linker in CA-4 was replaced with the azetidin-2-one ring aiming to prevent the cis/trans isomerization that suppresses the activity of CA-4, thereby enhancing its antiproliferative activity. All new compounds were investigated in vitro against MCF-7 and HCT-116 cell lines. The inhibition of tubulin polymerization by four most potent compounds 8g, 8j, 8n and 8o was also evaluated. The synthesis of the final targets was achieved adopting Staudinger reaction. Molecular modeling studies were performed to rationalize the biological results. � 2016, The Pharmaceutical Society of Korea.
Synthesis of novel S-acyl and S-alkylpyrimidinone derivatives as potential cytotoxic agents
(Springer Netherlands, 2016) Said M.M.; Taher A.T.; El-Nassan H.B.; El-Khouly E.A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; 33 Kasr El-Aini Street; Cairo; 11562; Egypt; Organic chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
Abstract: Two series of 4-phenyl-5-cyanopyrimidin-6-one derivatives bearing various S-alkyl or S-acyl moieties at position 2 were prepared as cytotoxic agents. All compounds were tested for possible anti-cancer activity on two cell lines (MCF-7 and HCT-116). The MCF-7 cell line was found to be more sensitive than the HCT-116 cell line to the action of the compounds. Compound 8g was the most potent on the MCF-7 cell line with IC50 18.3�nM/mL, whereas its IC50 on the normal cell line (MRC-5) was 64.38�nM/mL, indicating its safety and selectivity towards the MCF-7 cell line. On the other hand, compound 8d was the most potent compound on the HCT-116 cell line with IC50 23.8�nM/mL. Compound 8g was screened against five kinases. The compound showed selective inhibitory activity against pim1 kinase with IC50 11.62��M. Graphical Abstract: [Figure not available: see fulltext.] � 2016, Springer Science+Business Media Dordrecht.
Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking
(Academic Press Inc., 2019) Ahmed E.M.; Khalil N.A.; Taher A.T.; Refaey R.H.; Nissan Y.M.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October 6 University; Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt
Novel series of some triazolo[4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10?5 M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking. 2019 Elsevier Inc.