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Nasser Saad

Basic information

Name : Nasser Saad
Title: Professor of Pharmaceutical Chemistry
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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...

Education

Certificate Major University Year
PhD 2006
Masters Pharmaceutical Chemistry 2001
Bachelor Pharmaceutical Sciences 1996

Researches /Publications

Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Nasser Saad Mohamed Ismail

Adel A.-H. Abdel-Rahman, Amira K. F. Shaban, Ibrahim F. Nassar, Dina S. EL-Kady, Samy F. Mahmoud, Hanem M. Awad and Wael A. El-Sayed

01/06/2021

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-􀀀C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[30,20:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1,2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24,0.65, 0.50, and 0.93 _M, respectively, compared to roscovitine (IC50 0.394 _M). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 _M, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 _M, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

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Medicinal attributes of pyridine scaffold as anticancer targeting agents

Nasser Saad Mohamed Ismail

Esraa Ali Mohamed, Mohamed Hagras and Hanan Refaat

01/02/2021

Background: The heterocyclic compounds particularly pyridine displayed clinical and biological implementation. Pyridine scaffolds have been detected in most relevant drug molecules that included pyridine provided a great possibility for treatment. Main text: Pyridine-containing compounds have increasing importance for medicinal application as antiviral, anticholinesterase activities, antimalarial, antimicrobial, antidiabetic and anticancer. This has generated concern among researchers in synthesising a variety of pyridine derivatives. Conclusion: This review focuses on different pyridine targets as anticancer and their pharmacophoric elements controlling its activity.

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Design and Synthesis of New CDK2 Inhibitors Containing Thiazolone and Thiazolthione Scafold with Apoptotic Activity

Nasser Saad Mohamed Ismail

Nour E. A. Abd El-Sattar, Eman H. K. Badawy,Wafaa H. AbdEl-Hady, Mohamed I. Abo-Alkasem, Asmaa A. Mandour

01/01/2021

Cyclin dependent kinase 2 (CDK2) inhibition is a well-established strategy for treating cancer. Different series of novel thiazolone (1, 7-9) together with fused thiazolthione (2-6, and 10) derivatives were designed, then synthesized and evaluated for their biological inhibitory activity against CDK2. Additionally, the cytotoxicity of the new compounds was explored against breast and colon cancer cell lines. The novel thiazolone and the fused thiazolthione derivatives exhibited potent CDK2/cyclin A2 inhibitory effect of an IC50 values ranging 105.39-742.78 nM. Amongst them compounds 4 and 6 revealed highest IC50 of 105.39 and 139.27 nM, respectively. Most compounds showed significant inhibition on both breast cancer and colon cancer cell lines with IC50 range 0.54-5.26 and 0.83-278 µM, respectively. Further investigations involved flow cytometry analysis on MCF-7 cancer cell line for compounds 5 and 7 which resulted in arrest cell-cycle at two phases Pre G1/G2-M and re-enforced apoptosis via activation of caspase-7. Molecular modeling simulation of the designed compounds revealed that they were well fitted into CDK2 active site and their complexes were stabilized through the essential hydrogen bonding. Three dimensional quantitative structure activity relationship (3D QSAR) pharmacophore, and absorption, distribution, metabolism, excretion, and toxicity (ADMET) studies were also carried out showing proper pharmacokinetic and drug-likeness which aided in the prediction of the structure requirements responsible for the observed antitumor activity.

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Discovery of pyrano [2,3- d] pyrimidine -2,4-dione derivatives as novel PARP-1 inhibitors: design, synthesis and antitumor activity

Nasser Saad Mohamed Ismail

Nour E. A. Abd El-sattar, Eman H. K. Badawy,Eman Z. Elrazaz

01/01/2021

Poly(ADP-ribose) polymerases-1 (PARP-1) are involved in DNA repair damage and so PARP-1 inhibitors have been used as potentiators in combination with DNA damaging cytotoxic agents to compromise the cancer cell DNA repair mechanism, resulting in genomic dysfunction and cell death. In this study, we report the synthesis of a novel series of pyrano[2,3-d]pyrimidine-2,4-dione analogues as potential inhibitors against PARP-1. All the newly synthesized compounds were evaluated for their inhibitory activity towards PARP-1 and examined for their anti-proliferative activity against MCF-7 and HCT116 human cancer cell lines. The synthesized compounds showed promising activity where compounds S2 and S7 emerged as the most potent PARP-1 inhibitors with an IC50 value of 4.06 ± 0.18 and 3.61 ± 0.15 nM, respectively compared to that of Olaparib 5.77 nM and high cytotoxicity against MCF-7 with IC50 2.65 ± 0.05 and 1.28 ± 1.12 μM, respectively (Staurosporine 7.258 μM). Compound S8 remarkably showed the highest cell growth inhibition against MCF-7 and HCT116 with an IC50 value of 0.66 ± 0.05 and 2.76 ± 0.06 μM, respectively. Furthermore, molecular docking of the compounds into the PARP-1 active site was performed to explore the probable binding mode. Finally, most of the synthesized compounds were predicted to have good pharmacokinetics properties in a theoretical kinetic study.

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Alkaloids: Therapeutic Potential against Human Coronaviruses

Nasser Saad Mohamed Ismail

Burtram C. Fielding , Carlos da Silva Maia Bezerra Filho and Damião Pergentino de Sousa

01/11/2020

Alkaloids are a class of natural products known to have wide pharmacological activity and have great potential for the development of new drugs to treat a wide array of pathologies. Some alkaloids have antiviral activity and/or have been used as prototypes in the development of synthetic antiviral drugs. In this study, eleven anti-coronavirus alkaloids were identified from the scientific literature and their potential therapeutic value against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is discussed. In this study, in silico studies showed an a_nity of the alkaloids for binding to the receptor-binding domain of the SARS-CoV-2 spike protein, putatively preventing it from binding to the host cell. Lastly, several mechanisms for the known anti-coronavirus activity of alkaloids were discussed, showing that the alkaloids are interesting compounds with potential use as bioactive agents against SARS-CoV-2.

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A Molecular Docking Study Repurposes FDA Approved Iron Oxide Nanoparticles to Treat and Control COVID-19 Infection

Nasser Saad Mohamed Ismail

Yasmin Abo-zeida, Gary R. McLeanc,d, Nadia M. Hamdye

01/07/2020

COVID-19, is a disease resulting from the SARS-CoV-2 global pandemic. Due to the current global emergency and the length of time required to develop specific antiviral agent(s) and a vaccine for SARS-CoV-2, the world health organization (WHO) adopted the strategy of repurposing existing medications to treat COVID-19. Iron oxide nanoparticles (IONPs) were previously approved by the US food and drug administration (FDA) for anemia treatment and studies have also demonstrated its antiviral activity in vitro. Therefore, we performed a docking study to explore the interaction of IONPs (Fe2O3 and Fe3O4) with the spike protein receptor binding domain (S1-RBD) of SARS-CoV-2 that is required for virus attachment to the host cell receptors. A similar docking analysis was also performed with hepatitis C virus (HCV) glycoproteins E1 and E2. These studies revealed that both Fe2O3 and Fe3O4 interacted efficiently with the SARS-CoV-2 S1-RBD and to HCV glycoproteins, E1 and E2. Fe3O4 formed a more stable complex with S1-RBD whereas Fe2O3 favored HCV E1 and E2. These interactions of IONPs are expected to be associated with viral proteins conformational changes and hence, viral inactivation. Therefore, we recommend FDA-approved-IONPs to proceed for COVID-19 treatment clinical trials.

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Therapeutic Potential of Vanillin and its Main Metabolites to Regulate the Inflammatory Response and Oxidative Stress.

Nasser Saad Mohamed Ismail

Carlos S. M. Bezerra-Filho, Joice N. Barboza, Marilia T. S. Souza,Damião Pergentino de Sousa,

01/12/2019

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Towards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact of hinge interaction, and accessibility of their bioactive conformation on VEGFR-2 activities

Nasser Saad Mohamed Ismail

.Maiy Y. Jaballah, Rabah A. T. Serya, Sohair M. Khojah, Marawan Ahmed, Khaled Barakat & Khaled A. M. Abouzid

01/09/2019

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Towards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact on hinge interaction, and accessibility of their bioactive confirmation on VEGFR-2 activities

Nasser Saad Mohamed Ismail

Maiy Y. Jaballah, Rabah A. T. Serya, Sohair M. Khojah, Marawan Ahmed, Khaled Barakat & Khaled A. M. Abouzid

01/09/2019

Pyridazine scaffolds are considered privileged structures pertaining to its novelty, chemical stability, and synthetic feasibility. In our quest towards the development of novel scaffolds for effective vascular endothelial growth 2 (VEGFR-2) inhibition with antiangiogenic activity, four novel series of pyridazines were designed and synthesised. Five of the synthesised compounds; namely (8c, 8f, 15, 18b, and 18c) exhibited potent VEGFR-2 inhibitory potency (>80%); with IC50 values ranging from low micromolar to nanomolar range; namely compounds 8c, 8f, 15, 18c with (1.8 µM, 1.3 µM, 1.4 µM, 107 nM), respectively. Moreover, 3-[4-{(6-oxo-1,6-dihydropyridazin-3-yl)oxy}phenyl]urea derivative (18b) exhibited nanomolar potency towards VEGFR-2 (60.7 nM). In cellular assay, the above compounds showed excellent inhibition of VEGF-stimulated proliferation of human umbilical vein endothelial cells at 10 μM concentration. Finally, an extensive molecular simulation study was performed to investigate the probable interaction with VEGFR-2.

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Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo[1,5-a] pyrimidine scaffold with apoptotic activity

Nasser Saad Mohamed Ismail

Diaa A. Ibrahim, Amira M. Elmetwali, Ghada M.E. Ali

01/05/2019

Different series of novel pyrazole and pyrazolo[1,5-a] pyrimidine derivatives (2a-g), (3a-c), (7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit CDK2/cyclin A2 enzyme in vitro. In addition, the cytotoxicity of the newly synthesized compounds was screened against four different human cancer cell lines. The CDK2/cyclin A2 enzyme inhibitory activity revealed that compounds (2d) and (2 g) are among the most active with inhibitory activity values of 60% and 40%, respectively, while compounds (7d) and (10b) exhibited the highest activity among the newly synthesized derivatives against four tumor cell lines (HepG2, MCF-7, A549 and Caco2) with IC50 values 24.24, 14.12, 30.03 and 29.27 μM and 17.12, 10.05, 29.95 and 25.24 μM, respectively. Flow cytometry cell cycle assay was carried for compounds (7d) and (10b) to investigate their apoptotic activity. The obtained results revealed that they induced cell-cycle arrest in the G0-G1phase and reinforced apoptotic DNA fragmentation. Molecular modeling studies have been carried out to gain further understanding the binding mode of the target compounds together with field alignment to define the similar field properties.

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Design, synthesis and molecular modeling study of certain VEGFR-2 inhibitors based on thienopyrimidine scaffold as cancer targeting agents

Nasser Saad Mohamed Ismail

Khaled A.M. Abouzid

01/03/2019

Different series of novel thieno [2,3-d]pyrimidine derivative (9a-d,10a-f,l,m and 15a-m) were designed, synthesized and evaluated for their ability to in vitro inhibit VEGFR-2 enzyme. Also, the cytotoxicity of the final compounds was tested against a panel of 60 different human cancer cell lines by NCI. The VEGFR-2 enzyme inhibitory results revealed that compounds 10d, 15d and 15 g are among the most active inhibitors with IC50 values of 2.5, 5.48 and 2.27 µM respectively, while compound 10a remarkably showed the highest cell growth inhibition with mean growth inhibition (GI) percent of 31.57%. It exhibited broad spectrum anti-proliferative activity against several NCI cell lines specifically on human breast cancer (T7-47D) and renal cancer (A498) cell lines of 85.5% and 77.65% inhibition respectively. To investigate the mechanistic aspects underlying the activity, further biological studies like flow cytometry cell cycle together with caspase-3 colorimetric assays were carried on compound 10a. Flow cytometric analysis on both MCV-7 and PC-3 cancer cells revealed that it induced cell-cycle arrest in the G0-G1phase and reinforced apoptosis via activation of caspase-3. Furthermore, molecular modeling studies have been carried out to gain further understanding of the binding mode in the active site of VEGFR-2 enzyme and predict pharmacokinetic properties of all the synthesized inhibitors.

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Design and synthesis of new Quinoxaline derivative as anticancer agent and apoptotic inducer

Nasser Saad Mohamed Ismail

Aliya M. S. El Newahie , Yassin M. Nissan , Dalal A. Abou El Ella , Sohair M. Khojah and Khaled A.M. Abouzid

01/03/2019

The quinoxaline scaffold is a promising platform for the discovery of active chemotherapeutic agents. Three series of quinoxaline derivatives were synthesized and biologically evaluated against three tumor cell lines (HCT116 human colon carcinoma, HepG2, liver hepatocellular carcinoma and MCF-7, human breast adenocarcinoma cell line), in addition to VEGFR-2 enzyme inhibition activity. Compounds VIId, VIIIa, VIIIc, VIIIe and XVa exhibited promising activity against the tested cell lines and weak activity against VEGFR-2. Compound VIIIc induced a significant disruption in the cell cycle profile and cell cycle arrest at the G2/M phase boundary. In further assays, the cytotoxic effect of the highly active compounds was determined using a normal Caucasian fibroblast-like fetal lung cell line (WI-38). Compound VIIIc could be considered as a lead compound that merits further optimization and development as an anti-cancer and an apoptotic inducing candidate against the HCT116 cell line

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Therapeutic potential of Vanillin and its main metabolites to regulate the inflammatory response and oxidative stress

Nasser Saad Mohamed Ismail

Peter Sabry, Marilia T.S.Souza, Joice N.Barboza, Carlos S.M. Bezzaro

01/03/2019

Many phenolic compounds found in foods and medicinal plants have shown interesting therapeutic potential and have attracted the attention of the pharmaceutical industry as promising pharmacologically active compounds in health promotion and disease prevention. Vanillin is a phenolic aldehyde, widely used as a flavoring agent in the food, pharmaceutical, and cosmetics industries. A variety of pharmacological activities has been attributed to this compound and its main metabolites, vanillic acid and vanillyl alcohol, including their anti-inflammatory ability. The relationship of the anti-inflammatory effects of vanillin, vanillic acid, and vanillyl alcohol and their actions on oxidative stress is well established. Considering that the inflammatory process is related to several pathologies, including new diseases with few therapeutic options, and limited efficiency, the search for effective treatment strategies and discovery of new anti-inflammatory agents capable of modulating inflammation becomes necessary. Therefore, in this review we discuss the therapeutic potential of vanillin and its main metabolites for the treatment of inflammatory diseases and their actions on redox status. In addition, the molecular docking evaluation of vanillin, its metabolites and isoeugenol was carried out into the phospholipase A2 binding site.

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Design, synthesis and 3D QSAR based pharmacophore study of novel imatinib analogs as antitumor-apoptotic agents

Nasser Saad Mohamed Ismail

Deena S Lasheen, Khaled AM Abouzid

01/05/2018

Aim: Imatinib possesses various mechanisms for combating cancer, making the development of imatinib analogs an attractive target for cancer research. Method: Two series of analogs were designed and synthesized, maintaining the essential pharmacophoric features in imatinib structure. The synthesized compounds were subjected to cell-based antiproliferative assays against nonsmall lung (A549) and colon cancer cell lines. In addition, flow cytometry cell cycle and caspase-3 colorimetric assays were performed. Results: Most compounds showed potent anticancer activity against both cell lines with IC50 = 0.14–5.07 μM. Three compounds demonstrated ability to reinforce cell cycle arrest at G1 stage in a manner similar to imatinib. In addition, they induced apoptosis via activation of caspase-3.

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Synthesis, characterization, and evaluation of cytotoxic effects of novel hybrid steroidal heterocycles as peg based nanoparticles.

Nasser Saad Mohamed Ismail

Mervat M Abd Elhalim, Shaymaa M M Yahya, Yasmin Y Omar, Ahmed A Abd Rabou, Deena S Lasheen, Mahmoud F Zawrah, Gamal A Elmegeed,

01/07/2017

Anticancer agents featuring hybrid molecules can improve effectiveness and diminish drug resistance. The current study aimed to introduce newly synthesized heterocyclic steroids of promising anticancer effects loaded in polyethylene glycol (PEG)•based nanoparticles form. Several heterocyclic steroids (1-9) were synthesized via multicomponent reactions (MCRs) and confirmed via the analytical and spectral data. Compounds 1, 2, 3, 4, 5, 6, 7 and 9, were investigated individually in their free and PEG based nano-size hybrid forms as anticancer agents against three human cell lines: hepatocellular carcinoma cells (HepG2); breast cancer cells (MCF-7); and colon cancer cells (HCT116). The neutral red supravital dye uptake assay was employed. Compound 6 in its PEG based nano-size form exhibited the best cytotoxic effects against HepG2 and HCT116 cell lines, with IC50 values of 2.44 µmol/l and 2.59 µmol/l, respectively. In addition, it demonstrated a low IC50 value against MCF-7 (3.46µmol/l) cells. This study introduced promising anticancer agents acting through conversion into PEG-based nanoparticles.

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Medicinal attributes of thienopyrimidine based scaffold targeting tyrosine kinases and their potential anticancer activities.

Nasser Saad Mohamed Ismail

Khaled A.M. Abouzid

01/07/2017

Thienopyrimidines (TP), comprising a thiophene ring fused with pyrimidine, are famous bioisosteres to purines, an essential part of the human metabolome. This scaffold has become an interesting structural element in the development of pharmaceutical compounds, due to their wide spectrum applications as cytotoxic agents against different types of human cancer cell lines, cGMP phosphodiesterase inhibitors, and anti‐viral, anti‐inflammatory, and anti‐microbial agents. The structural similarity of this scaffold with adenine made it an excellent moiety to be used in the design of kinase inhibitors. This review focuses on the chemistry of thienopyrimidine derivatives, their potential activities against various kinases, and their structure–activity relationship studies.

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Design, synthesis and anticancer evaluation of novel pyrazole, pyrazolo [3, 4-d] pyrimidine and their glycoside derivatives; Nucleosides.

Nasser Saad Mohamed Ismail

Nassar, Ibrahim F., Ahmed F. El Farargy, Fathy M. Abdelrazek,

01/03/2017

The chalcone derivatives 3a,b were cyclized upon reaction with thiourea to give the pyrazolo[3,4-d]pyrimidine derivatives 5a,b. Condensation of 5a,b and their hydrazide derivatives 8a,b with cyclic and acyclic glucose gave the condensed S- and N-glycosides 7a,b and 9a,b, respectively. Reaction of 3b with ethyl cyanoacetate followed by reaction with cyclic glucose afforded a mixture of the O- and/or N-glycoside isomers 12 and 13, respectively. The pyrazolo[3,4-c]pyrazole derivative 14 was also obtained from the reaction of 3b with hydrazine hydrate. A number of the synthesized compounds were screened for their antitumor activity against three different tumor cell lines HEPG2 (liver), HCT116 (colon) and MCF-7 (breast) with a docking study against CDK2.

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A study of the allosteric inhibition of HCV RNA-dependent RNA polymerase and implementing virtual screening for the selection of promising dual-site inhibitors with low resistance potential

Nasser Saad Mohamed Ismail

Heba S. A. Elzahabi, Peter Sabry, Fady N. Baselious, Andrew Samy AbdelMalak, Fady Hanna

01/01/2017

Structure-based pharmacophores were generated and validated using the bioactive conformations of different co-crystallized enzyme-inhibitor complexes for allosteric palm-1 and thumb-2 inhibitors of NS5B. Two pharmacophore models were obtained, one for palm-1 inhibitors with sensitivity = 0.929 and specificity = 0.983, and the other for thumb-2 inhibitors with sensitivity = 1 and specificity = 0.979. In addition, a quantitative structure activity relationship (QSAR) models were developed based on using the values of different scoring functions as descriptors predicting the activity on both allosteric binding sites (palm-1 and thumb-2). QSAR studies revealed good predictive and statistically significant two descriptor models (r2 = .837, r2adjusted = .792 and r2prediction = .688 for palm-1 model and r2 = .927, r2adjusted = .908 and r2prediction = .779 for thumb-2 model). External validation for the QSAR models assured their prediction power with r2ext = .72 and .89 for palm-1 and thumb-2, respectively. Different docking protocols were examined for their validity to predict the correct binding poses of inhibitors inside their respective binding sites. Virtual screening was carried out on ZINC database using the generated pharmacophores, the selected valid docking algorithms and QSAR models to find compounds that could theoretically bind to both sites simultaneously.

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Rational design, synthesis and 2D-QSAR studies of antiproliferative tropane-based compounds†

Nasser Saad Mohamed Ismail

Riham F. George, Rabah A. T. Serya, Fady N. Baselious, May El-Manawaty, ElSayed M. Shalaby and Adel S. Girgis

01/10/2016

3,4-Diaryl-11-methyl-7-[(aryl)methylidene]-4,5,11-triazatricyclo[6.2.1.0*2,6*]undec-5-enes 14a–s were synthesized through reaction of 2,4-bis[(aryl)methylidene]-8-methyl-8-azabicyclo[3.2.1]octan-3-ones 12a–f with aryl hydrazines in the presence of catalytic amount of thiamine hydrochloride. Meanwhile, the 4-acetyl analogs 16a,b were obtained through reaction of 12b,e and hydrazine hydrate in acetic acid. Good support for the structure was received from single crystal X-ray studies of 14a. Some of the synthesized tropane containing-compounds showed promising antitumor properties during the in vitro MTT bio-assay against HepG2 (hepatocellular) and MCF7 (breast) human tumor carcinoma cell lines, with potency higher than that of doxorubicin (DNA intercalating agent, standard reference). Statistically significant 2D-QSAR model describes the antitumor properties against MCF7.

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Medicinal attributes of pyrazolo[1,5-a]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Nasser Saad Mohamed Ismail

Ghada M.E. Ali, Diaa A. Ibrahim, Amira M. Elmetwali

01/08/2016

Pyrazolo pyrimidines are fused heterocyclic ring systems which known as bioisosteres of adenine, that are necessary for every aspect of cell life. Pyrazolo[1,5- a]pyrimidines derivatives have been explored for their inhibitory activity towards a variety of protein kinase enzymes and their function as anticancer agents. This review to the best of our knowledge is the first assemblage on synthesis and medicinal aspects including structure activity relationships of pyrazolo[1,5-a]pyrimidines reported to date.

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Effect of methyl-Β-cyclodextrin complexation on the hypoglycemic and hypolipidemic effects of khellin

Nasser Saad Mohamed Ismail

MONA M. ABOUSAMRA, MONA BASHA, SALLY EL AWDAN

01/07/2016

Objective: The present work tackled the development and evaluation of inclusion complex of khellin (KH) and methyl-β-cyclodextrin (MβCD). In addition, it tested its possible hypoglycemic and hypolipidemic effects. Methods: Inclusion complexes of KH-MβCD in the presence of water-soluble polymer were prepared by freeze drying (FD), co-evaporation (EV) and kneading methods (KN). The selected ternary complex was characterized by Fourier transform infrared spectrophotometry (FTIR), x-ray diffractometry (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy [1]. Assessment of the hypoglycemic effect of the selected ternary complex versus the standard drug metformin was studied. Two different doses of the ternary complex were administered orally to streptozotocin (STZ)-induced type 2diabetic rats. Their hypoglycemic and hypolipidemic effects were evaluated by measuring the fasting blood glucose level (BGL), total cholesterol (TC) and triglycerides levels (TG) along the study period. Results: The FD complex showed the highest drug dissolution rate. All the performed characterization analysis confirmed the formation of a KHMβCD inclusion complex. The in vivo study declared that both doses showed a marked hypoglycemic and hypolipidemic effects compared to metformin. Conclusion: In conclusion, this study points for the first time that the complexation of KH with MβCD could notably improve the dissolution rate and hence the bioavailability of KH. Moreover, this study demonstrated that this compound has a hypoglycemic and hypolipidemic effect. Thus, it can

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Effect of methyl-Β-cyclodextrin complexation on the hypoglycemic and hypolipidemic effects of khellin

Nasser Saad Mohamed Ismail

MONA M. ABOUSAMRA, MONA BASHA, SALLY EL AWDAN

01/07/2016

Objective: The present work tackled the development and evaluation of inclusion complex of khellin (KH) and methyl-β-cyclodextrin (MβCD). In addition, it tested its possible hypoglycemic and hypolipidemic effects. Methods: Inclusion complexes of KH-MβCD in the presence of water-soluble polymer were prepared by freeze drying (FD), co-evaporation (EV) and kneading methods (KN). The selected ternary complex was characterized by Fourier transform infrared spectrophotometry (FTIR), x-ray diffractometry (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy [1]. Assessment of the hypoglycemic effect of the selected ternary complex versus the standard drug metformin was studied. Two different doses of the ternary complex were administered orally to streptozotocin (STZ)-induced type 2diabetic rats. Their hypoglycemic and hypolipidemic effects were evaluated by measuring the fasting blood glucose level (BGL), total cholesterol (TC) and triglycerides levels (TG) along the study period. Results: The FD complex showed the highest drug dissolution rate. All the performed characterization analysis confirmed the formation of a KHMβCD inclusion complex. The in vivo study declared that both doses showed a marked hypoglycemic and hypolipidemic effects compared to metformin. Conclusion: In conclusion, this study points for the first time that the complexation of KH with MβCD could notably improve the dissolution rate and hence the bioavailability of KH. Moreover, this study demonstrated that this compound has a hypoglycemic and hypolipidemic effect. Thus, it can

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Quinoxaline-Based Scaffolds Targeting Tyrosine Kinases and Their Potential Anticancer Activity

Nasser Saad Mohamed Ismail

Aliya M. S. El Newahie, Dalal A. Abou El Ella, and Khaled A. M. Abouzid

01/03/2016

Quinoxaline derivatives, also called benzopyrazines, are an important class of heterocyclic compounds. Quinoxalines have drawn great attention due to their wide spectrum of biological activities. They are considered as an important basis for anticancer drugs due to their potential activity as protein kinase inhibitors. In this review, we focus on the chemistry of the quinoxaline derivatives, the strategies for their synthesis, their potential activities against various tyrosine kinases, and on the structure–activity relationship studies reported to date.

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Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Nasser Saad Mohamed Ismail

Eslam M.H. Ali d, 1, Diaa A. Ibrahim c, Rabah A.T. Serya, Dalal A. Abou El Ella

01/03/2016

Pyrazolopyrimidines are fused heterocyclic ring systems which structurally can consider as bioisosteres of adenine, which is fundamental for every aspect of cell life. Pyrazolo[3,4-d]pyrimidines derivatives have been explored for their inhibitory activity towards various protein kinase enzymes and their role as anticancer agents. The present review to the best of our knowledge is the first compilation on synthesis and medicinal aspects including structureeactivity relationships of pyrazolo[3,4-d]pyrimidines reported to date.

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Recent advances in 4-aminoquinazoline based scaffold derivatives targeting EGFR kinases as anticancer agents

Nasser Saad Mohamed Ismail

Rania S.M. Ismail, Sahar Abuserii d, Dalal A. Abou El Ella c

01/03/2016

Quinazoline derivatives are fused heterocyclic ring systems which have been explored for their inhibitory activity towards various protein kinase enzymes and their role as anticancer agents. The present review to represent the most recent synthetic strategies and medicinal aspects including structure activity relationships of substituted quinazolines as EGFR inhibitors reported to date.

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Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases

Nasser Saad Mohamed Ismail

Nasser S.M. Ismail *, Eslam M.H. Ali , Diaa A. Ibrahim , Rabah A.T. Serya ,

01/03/2016

Pyrazolopyrimidines are fused heterocyclic ring systems which structurally can consider as bioisosteres of adenine, which is fundamental for every aspect of cell life. Pyrazolo[3,4-d]pyrimidines derivatives have been explored for their inhibitory activity towards various protein kinase enzymes and their role as anticancer agents. The present review to the best of our knowledge is the first compilation on synthesis and medicinal aspects including structureeactivity relationships of pyrazolo[3,4-d]pyrimidines reported to date.

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Recent advances in 4-aminoquinazoline based scaffold derivatives targeting EGFR

Nasser Saad Mohamed Ismail

Rania S.M. Ismail, Nasser S.M. Ismail, Sahar abuserii, Dalal. A. Abou El Ella

01/02/2016

Quinazoline derivatives are fused heterocyclic ring systems which have been explored for their inhibitory activity towards various protein kinase enzymes and their role as anticancer agents. The present review to represent the most recent synthetic strategies and medicinal aspects including structure activity relationships of substituted quinazolines as EGFR inhibitors reported to date.

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

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,

01/11/2015

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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Synthesis, and QSAR analysis of anti-oncological active spiro-alkaloids

Nasser Saad Mohamed Ismail

Adel S. Girgis, Siva S. Panda, I. S. Ahmed Farag, A. M. El-Shabiny, A. M. Moustafa, Nasser S. M. Ismail, Girinath G. Pillai, Chandramukhi S. Panda, Dennis Hall, and Alan R. Katritzky,

01/03/2015

3D-pharmacophore and 2D-QSAR modeling studies describe the anti-oncological properties of spiroalkaloids. The dispiro[2H-indene-2,3’-pyrrolidine-2’,3’’-[3H]indole]-1,2’’(1’’H, 3H)-diones 20–38 were prepared via 1,3-dipolar cycloaddition reactions of azomethine ylides (generated in situ via decarboxylative condensation of isatins 7–9 with sarcosine 10) and 2-(arylmethylidene)-2,3-dihydro-1H-inden-1-ones 11–19 in refluxing ethanol. Some of the spiro-alkaloids (21, 22, 29 and 37) revealed potent antitumor properties against melanoma carcinoma cell lines (GaLa, LuPiCi and LuCa) utilizing the in vitro SRB standard method exhibiting potency close to that of the standard reference doxorubicin.

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