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Nasser Saad

Basic information

Name : Nasser Saad
Title: Associate Professor of Pharmaceutical Chemistry
Google Schoolar Link: http://scholar.google.com.eg/citations?hl=en&user=Ja7kt4oAAAAJ&view_op=list_works
Personal Info: Dr. Nasser Saad Mohamed Ismail, Ass. prof of Pharmaceutical Chemistry - Department of Pharmaceutical Chemistry. He has a PH.D and MSC degree from Ain Shams university. He received PH.D from Ain Sham University, March 2006 and Associate Professor of Pharmaceutical Chemistry April 2011. View More...


Certificate Major University Year
PhD Pharmaceutical Chemistry Ain Shams University 2006
Masters Pharmaceutical Chemistry Ain Shams University - Pharmaceutical Chemistry 2001
Bachelor Pharmaceutical Sciences Zagazig University _ Faculty of Pharmaceuitical Scince 1996

Teaching Experience

Name of Organization Position From Date To Date
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University. Demonstrator 01/11/1996 01/02/2001
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University Lecturer 01/03/2006 01/04/2011
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University Assistant Lecturer 01/03/2001 01/02/2006
Faculty of Pharmacy, Future University associate professor of Pharmaceutical Chemistry 01/01/2014 01/01/2016

Researches /Publications

Development of Potent Adenosine Monophosphate - 01/1

Nasser Saad Mohamed Ismail

Eman M. E. Dokla,[a, b] Chun-Sheng Fang,[a] Po-Ting Lai,[a] Samuel K. Kulp,[a]


Previously, we reported the identification of a thiazolidinedione- based adenosine monophosphate activated protein kinase (AMPK) activator, compound 1 (N-[4-({3-[(1-methylcyclohexyl) methyl]-2,4-dioxothiazolidin-5-ylidene}methyl)phenyl]-4- nitro-3-(trifluoromethyl)benzenesulfonamide), which provided a proof of concept to delineate the intricate role of AMPK in regulating oncogenic signaling pathways associated with cell proliferation and epithelial–mesenchymal transition (EMT) in cancer cells. In this study, we used 1 as a scaffold to conduct lead optimization, which generated a series of derivatives. Analysis of the antiproliferative and AMPK-activating activities of individual derivatives revealed a distinct structure–activity relationship and identified 59 (N-(3-nitrophenyl)-N’-{4-[(3-{[3,5- bis(trifluoromethyl)phenyl]methyl}-2,4-dioxothiazolidin-5-ylidene) methyl]phenyl}urea) as the optimal agent. Relative to 1, compound 59 exhibits multifold higher potency in upregulating AMPK phosphorylation in various cell lines irrespective of their liver kinase B1 (LKB1) functional status, accompanied by parallel changes in the phosphorylation/expression levels of p70S6K, Akt, Foxo3a, and EMT-associated markers. Consistent with its predicted activity against tumors with activated Akt status, orally administered 59 was efficacious in suppressing the growth of phosphatase and tensin homologue (PTEN)-null PC-3 xenograft tumors in nude mice. Together, these findings suggest that 59 has clinical value in therapeutic strategies for PTEN-negative cancer and warrants continued investigation in this regard.

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Thieno[2,3-d]pyrimidine based derivatives as kinase inhibitors and anticancer agents, - 01/1

Nasser Saad Mohamed Ismail

Eman Z. Elrazaz, Rabah A.T. Serya, Nasser S.M. Ismail, Dalal A. Abou El Ella, Khaled A.M. Abouzid


Thienopyrimidines are fused heterocyclic ring systems; structurally resemble purines, exerting pharmacological potential in different aspects. They are known to play a crucial role in various disease conditions. Thieno[2,3-d]pyrimidine derivatives have been explored for their inhibitory activities towards various protein kinase enzymes. The present review is a compilation on chemical synthesis and biological anticancer significance, via inhibition of specific protein kinase enzymes, including structure eactivity relationships of thieno[2,3-d]pyrimidines derivatives reported to date.

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Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents, - 01/1

Nasser Saad Mohamed Ismail

Hany S. Ibrahim, Sahar M. Abou-seri , Nasser S.M. Ismail, Mahmoud M. Elaasser, Mohamed H. Aly, Hatem A. Abdel-Aziz,


Many bis-isatins and isatins with hydrazide extension were reported to have a potential anti-proliferative effects against different cancer cell lines and cancer targets. In this study, four series of bis-isatins with hydrazide linkers were synthesized. These compounds were investigated for their antitumor activity by assessing their cytotoxic potency against HepG2, MCF-7 and HCT-116 cancer cell lines. Compound 21c possessed significant cytotoxic activity against MCF-7 (IC50 ¼ 1.84 mM) and HCT-116 (IC50 ¼ 3.31 mM) that surpasses the activity of doxorubicin against both cell lines (MCF-7; IC50 ¼ 2.57 mM and HCT-116; IC50 ¼ 3.70 mM). Cell cycle analysis and annexin V-FITC staining of MCF-7 cells treated with 21c suggested that the cytotoxic effect of the compound could be attributed to its pro-apoptotic activity.

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Design, synthesis and biological evaluation of novel quinazoline -based anti-inflammatory agents acting as PDE4B inhibitors - 01/1

Nasser Saad Mohamed Ismail

Rabah A. T. Syria, Abeer Abd el hafez, Dalal A. Abou El Ella, Nasser S.M. Ismail


A novel series of quinzoline based compounds (IIIa–d, VIa–f, IXa–f) were designed, synthesized and screened for their inhibitory activity towards the PDE4B isoform. The in vivo anti-inflammatory effect of the titled compounds (IIIa–d, VIa–f, IXa–f) as well as their effect on the level of tumor necrosis factor (TNF-α) were evaluated. Among all of the synthesized compounds, IXb, IXd and IXf, exhibited good inhibitory activity against PDE4B enzyme with inhibition percentages of 42, 62 and 68%, respectively. Most of the tested compounds showed potent anti-inflammatory activity compared to indomethacin with a marked decrease in TNF-α level. The ulcerogenic effect of the tested compounds was also examined. The gastric mucosa of the tested animals remained intact after oral administration of the hit compounds. Additionally, docking study was used to explore the possible binding mode of the active compounds on the PDE4B enzyme as well as to illustrate the selectivity of the active hits on the PDE4B isoform.

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Synthesis and in vitro antiproliferative activity of novel pyrazolo[3,4-d]pyrimidine derivatives, - 01/0

Nasser Saad Mohamed Ismail

Nermin S. Abdou, Rabah A. T. Serya, Ahmed Esmat, Mai F. Tolba, Nasser S. M. Ismail and Khaled A. M. Abouzid


A novel series of pyrazoloij3,4-d]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity. Among the five compounds selected by NCI, compound 11a showed a distinctive pattern of selectivity on cell line panels and was further screened for a 5-log dose range, where it showed potent antiproliferative activity with median growth inhibition (GI50) equal to 1.71 μM against the CNS cancer SNB-75 cell line. The tested derivative showed remarkably the highest cell growth inhibition against non-small cell lung cancer HOP-62, CNS cancer SNB-75, breast cancer HS578T, and melanoma MALME- 3M cell lines. Flow cytometric analysis revealed that compound 11a could significantly induce apoptosis in A549 cells in vitro at low micromolar concentrations. Further investigation showed that compound 11a induced significant cell cycle arrest at G0/G1 phase partly due to its ability to downregulate cyclin D1 and upregulate p27kip1 levels

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