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Author Adnan A Bekhit

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Investigation of the anti-inflammatory and analgesic activities of promising pyrazole derivative.

Adnan A Bekhit, Sherry N Nasralla, Eman J El-Agroudy, Nahla Hamouda, Ahmed Abd El-Fattah, Salma A Bekhit, Kikuko Amagase, Tamer M Ibrahim,

The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital importance to patients suffering from chronic course pain and inflammatory conditions. This study aims at evaluating the therapeutic activity and adverse drug reactions associated with the use ... Read more >>

Eur J Pharm Sci (European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences)
[2022, 168:106080]

Cited: 0 times

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Design and synthesis of 2-Substituted-4-benzyl-5-methylimidazoles as new potential Anti-breast cancer agents to inhibit oncogenic STAT3 functions.

Botros Y Beshay, Amira A Abdellatef, Yasser M Loksha, Salwa M Fahmy, Nargues S Habib, Alaa El-Din A Bekhit, Paris E Georghiou, Yoshihiro Hayakawa, Adnan A Bekhit,

STAT3 signaling is known to be associated with tumorigenesis and further cancer cell-intrinsic activation of STAT3 leads to altered regulation of several oncogenic processes. Given the importance of STAT3 in cancer development and progression particularly breast cancer, it is crucial to discover new chemical entities of STAT3 inhibitor to develop ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 113:105033]

Cited: 0 times

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Potential anti-COVID-19 activity of Egyptian propolis using computational modeling

Bassma H Elwakil, Marwa M Shaaban, Adnan A Bekhit, Moustafa Y El-Naggar, Zakia A Olama,

Aim: To investigate the prospective anti COVID-19 activity of Egyptian propolis. Material & methods: Propolis samples were collected from different Egyptian geographical areas and characterized using standardized methods, scanning electron microscope and gas chromatography/mass spectrometry along with computational modeling to predict the anti-COVID-19 activity. Results & conclusion: Gas chromatography/mass spectrometry analysis ... Read more >>

Future Virol (Future virology)
[2021, :]

Cited: 0 times

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Design, synthesis, biological evaluation and in silico studies of certain aryl sulfonyl hydrazones conjugated with 1,3-diaryl pyrazoles as potent metallo-β-lactamase inhibitors.

Marwa M Shaaban, Hanan M Ragab, Kenichi Akaji, Ross P McGeary, Alaa-Eldin A Bekhit, Waleed M Hussein, Julia L Kurz, Bassma H Elwakil, Salma A Bekhit, Tamer M Ibrahim, Mona A Mahran, Adnan A Bekhit,

Based on a structure-guided approach, aryl sulfonyl hydrazones conjugated with 1,3-diaryl pyrazoles were designed to target metallo-β-lactamases (MBLs), using Klebsiella pneumoniaeNDM-1 as a model. The in vitro MBLs inhibition showed remarkable inhibition constant for most of the designed compounds at a low micromolar range (1.5-16.4 µM) against NDM-1, IMP-1 and AIM-1 ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 105:104386]

Cited: 1 time

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Combination of magnetic targeting with synergistic inhibition of NF-κB and glutathione via micellar drug nanomedicine enhances its anti-tumor efficacy.

Kholod A Elhasany, Sherine N Khattab, Adnan A Bekhit, Doaa M Ragab, Mohammad A Abdulkader, Amira Zaky, Maged W Helmy, Hayam M A Ashour, Mohamed Teleb, Nesreen S Haiba, Ahmed O Elzoghby,

Breast cancer is not only one of the most prevalent types of cancer, but also it is a prime cause of death in women aged between 20 and 59. Although chemotherapy is the most common therapy approach, multiple side effects can result from lack of specificity and the use of ... Read more >>

Eur J Pharm Biopharm (European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V)
[2020, 155:162-176]

Cited: 1 time

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Macroporous resin extraction of PHNQs from Evechinus chloroticus sea urchin and their in vitro antioxidant, anti-bacterial and in silico anti-inflammatory activities

Yakun Hou, Alan Carne, Michelle McConnell, Sonya Mros, Adnan A Bekhit, Alaa El-Din A Bekhit,

This study investigated the polyhydroxyl-1,4-naphthoquinone (PHNQ) composition and bioactivities of Evechinus chloroticus sea urchin shell and spine waste extracted using the macroporous resins NKA-9, D4020, D4006, and D101. The mineral and protein contents in the shell and spine were found to be 85.21% and 84.14%, 3.85% and 8.96%, respectively. Spine ... Read more >>

Lebensm Wiss Technol (Lebensmittel-Wissenschaft + [i.e. und] Technologie.)
[2020, 131:Not Available]

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Lactoferrin-dual drug nanoconjugate: Synergistic anti-tumor efficacy of docetaxel and the NF-κB inhibitor celastrol.

Mona A Abdelmoneem, Mahmoud M Abd Elwakil, Sherine N Khattab, Maged W Helmy, Adnan A Bekhit, Mohammad A Abdulkader, Amira Zaky, Mohamed Teleb, Kadria A Elkhodairy, Fernando Albericio, Ahmed O Elzoghby,

Despite the progress in cancer nanotherapeutics, some obstacles still impede the success of nanocarriers and hinder their clinical translation. Low drug loading, premature drug release, off-target toxicity and multi-drug resistance are among the most difficult challenges. Lactoferrin (LF) has demonstrated a great tumor targeting capacity via its high binding affinity ... Read more >>

Mater Sci Eng C Mater Biol Appl (Materials science & engineering. C, Materials for biological applications)
[2021, 118:111422]

Cited: 3 times

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Co-Administration of Tretinoin Enhances the Anti-Cancer Efficacy of Etoposide via Tumor-Targeted Green Nano-Micelles.

Mohamed Gaber, Kholod A Elhasany, Saly Sabra, Maged W Helmy, Jia-You Fang, Sherine N Khattab, Adnan A Bekhit, Mohamed Teleb, Kadria A Elkodairy, Ahmed O Elzoghby,

Herein we report promoted anti-cancer activity via a combination strategy of synergistic chemotherapy/retinoid-based breast cancer therapy with shell-stabilized micellar green nanomedicine. Amphiphilic zein-chondroitin sulfate (ChS)-based copolymeric micelles (PMs) were successfully developed via carbodiimide coupling for concomitant delivery of etoposide (ETP) and all-trans retinoic acid (ATRA) to breast cancer. The micelles ... Read more >>

Colloids Surf B Biointerfaces (Colloids and surfaces. B, Biointerfaces)
[2020, 192:110997]

Cited: 3 times

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Novel Siwa propolis and colistin-integrated chitosan nanoparticles: elaboration; in vitro and in vivo appraisal.

Yosra Sr Elnaggar, Bassma H Elwakil, Salma S Elshewemi, Moustafa Y El-Naggar, Adnan A Bekhit, Zakia A Olama,

Aim: The present study aimed to formulate novel cremophore-decorated chitosan nanoparticles of colistin, integrated with Siwa propolis extract, to solve bacterial resistance to colistin. Materials & methods: The novel nanoformula was prepared using an incorporation method. Physicochemical assessment and in vivo studies of the selected nanoformulations were performed. Results: The ... Read more >>

Nanomedicine (Lond) (Nanomedicine (London, England))
[2020, :]

Cited: 2 times

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In vitro antioxidant and antimicrobial activities, and in vivo anti-inflammatory activity of crude and fractionated PHNQs from sea urchin (Evechinus chloroticus).

Yakun Hou, Alan Carne, Michelle McConnell, Adnan A Bekhit, Sonya Mros, Kikuko Amagase, Alaa El-Din A Bekhit,

This study investigated the bioactivities of polyhydroxyl-1,4-naphthoquinone (PHNQ) extracts from Evechinus chloroticus shell waste. PHNQs were extracted from E. chloroticus shells and spines using different solvents and the crude extracts were fractionated by HPLC. The antioxidant activity of the PHNQ extracts were evaluated by the DPPH, ABTS, ORAC and FRAP ... Read more >>

Food Chem (Food chemistry)
[2020, 316:126339]

Cited: 1 time

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Synthesis, in vitro biological evaluation and in silico studies of certain arylnicotinic acids conjugated with aryl (thio)semicarbazides as a novel class of anti-leishmanial agents.

Wagdy M Eldehna, Hadia Almahli, Tamer M Ibrahim, Mohamed Fares, Tarfah Al-Warhi, Frank M Boeckler, Adnan A Bekhit, Hatem A Abdel-Aziz,

Herein we introduce new compounds as conjugates of arylnicotinic acids with aryl (thio)semicarbazide derivatives. Based on a structure-guided approach, they were designed to possess anti-leishmanial activity through anti-folate mechanism, via targeting Leishmania major pteridine reductase 1 (Lm-PTR1). The in vitro anti-promastigote and anti-amastigote activity were promising for many thiosemicarbazide derivatives and ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 179:335-346]

Cited: 2 times

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Design, synthesis and molecular modeling studies of new series of s-triazine derivatives as antimicrobial agents against multi-drug resistant clinical isolates.

Nesreen Saied Haiba, Hosam H Khalil, Mohamed Abdel Moniem, Marwa H El-Wakil, Adnan A Bekhit, Sherine Nabil Khattab,

Three novel series of s-triazine derivatives, including thirty-five new compounds 2a-d, 3a-3p, 4b-d, 5b-d, 6d-6d, and 7a-7f were synthesized comprising a diversity of substituents based on the structure of Astrazeneca arylaminotriazine DNA gyrase B inhibitor. The antimicrobial activity was determined for all compounds against Staphylococcus aureus, Escherichia coli and Candida ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 89:103013]

Cited: 1 time

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Synthesis, in silico experiments and biological evaluation of 1,3,4-trisubstituted pyrazole derivatives as antimalarial agents.

Adnan A Bekhit, Manal N Saudi, Ahmed M M Hassan, Salwa M Fahmy, Tamer M Ibrahim, Doaa Ghareeb, Aya M El-Seidy, Sherry N Nasralla, Alaa El-Din A Bekhit,

New 1,3,4-trisubstituted pyrazole derivatives were synthesized and evaluated for their antiplasmodial activity. Compounds 4b, 4c, 7a and 7d were the most potent antiplasmodial agents against P. berghei with percent of suppression ranging from 90 to 100%. They were also screened for their in vitro antimalarial activity against the chloroquine resistant strain P. falciparum, ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 163:353-366]

Cited: 4 times

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Leishmania treatment and prevention: Natural and synthesized drugs.

Adnan A Bekhit, Eman El-Agroudy, Aliaa Helmy, Tamer M Ibrahim, Amin Shavandi, Alaa El-Din A Bekhit,

Leishmaniasis affects over 150 million people all over the world, especially in subtropical regions. Currently used antileishmanial synthesized drugs are associated with some drawbacks such as resistance and cytotoxicity, which hamper the chances of treatment. Furthermore, effective leishmanial vaccines are not well developed. Promising chemotherapy, either from natural or synthetic ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 160:229-244]

Cited: 9 times

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Synthesis, molecular modeling and biological screening of some pyrazole derivatives as antileishmanial agents.

Adnan A Bekhit, Manal N Saudi, Ahmed Mm Hassan, Salwa M Fahmy, Tamer M Ibrahim, Doaa Ghareeb, Aya M El-Seidy, Sayed M Al-Qallaf, Huda J Habib, Alaa El-Din A Bekhit,

<h4>Aim</h4>Novel open chain and cyclized derivatives containing pyrazole scaffold were designed, synthesized and evaluated as antileishmanial compounds. Methodology & results: In silico reverse docking experiment suggested Leishmania major pteridine reductase (Lm-PTR1) as a putative target for the synthesized compounds. In vitro antileishmanial screening against L. major promastigotes and amastigotes using miltefosine ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2018, 10(19):2325-2344]

Cited: 1 time

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Lactobionic/Folate Dual-Targeted Amphiphilic Maltodextrin-Based Micelles for Targeted Codelivery of Sulfasalazine and Resveratrol to Hepatocellular Carcinoma.

Doaa M Anwar, Sherine N Khattab, Maged W Helmy, Mohamed K Kamal, Adnan A Bekhit, Kadria A Elkhodairy, Ahmed O Elzoghby,

In this study, promising approaches of dual-targeted micelles and drug-polymer conjugation were combined to enable injection of poorly soluble anticancer drugs together with site-specific drug release. Ursodeoxycholic acid (UDCA) as a hepatoprotective agent was grafted to maltodextrin (MD) via carbodiimide coupling to develop amphiphilic maltodextrin-ursodeoxycholic acid (MDCA)-based micelles. Sulfasalazine (SSZ), ... Read more >>

Bioconjug Chem (Bioconjugate chemistry)
[2018, 29(9):3026-3041]

Cited: 5 times

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Anti-leishmanial click modifiable thiosemicarbazones: Design, synthesis, biological evaluation and in silico studies.

Mohamed G Temraz, Perihan A Elzahhar, Alaa El-Din A Bekhit, Adnan A Bekhit, Hala F Labib, Ahmed S F Belal,

Leishmaniasis is a devastating tropical disease with limited therapeutic options. Depending on recently reported active anti-leishmanial compounds, we designed and synthesized a series of click modifiable 1,2,3-triazole and thiosemicarbazone hybrids. Most of the synthesized compounds showed comparable to superior activity to a well-established anti-leishmanial drug miltefosine. Compounds 2 and 10a ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 151:585-600]

Cited: 6 times

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Folate conjugated vs PEGylated phytosomal casein nanocarriers for codelivery of fungal- and herbal-derived anticancer drugs.

Shaymaa W El-Far, Maged W Helmy, Sherine N Khattab, Adnan A Bekhit, Ahmed A Hussein, Ahmed O Elzoghby,

<h4>Aim</h4>Monascin and ankaflavin, the major fractions of the fungal-derived monascus yellow pigments, were incorporated with the herbal drug, resveratrol (RSV) within the core of folate-conjugated casein micelles (FA-CAS MCs, F1) for active targeting. PEGylated RSV-phospholipid complex bilayer enveloping casein-loaded micelles (PEGPC-CAS MCs) were also developed as passive-targeted nanosystem.<h4>Results</h4>FA- and PEGPC-CAS ... Read more >>

Nanomedicine (Lond) (Nanomedicine (London, England))
[2018, 13(12):1463-1480]

Cited: 3 times

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1,3,5-Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity.

Sherine N Khattab, Hosam H Khalil, Adnan A Bekhit, Mohamed M Abd El-Rahman, Beatriz G de la Torre, Beatriz G de la Torre, Ayman El-Faham, Fernando Albericio,

A library of short di-, tri-, and tetra-peptides with an s-triazine moiety at the N terminus and either an amide or ethyl ester C terminus was prepared in solution and on the solid phase. The two remaining positions of the s-triazine moiety were substituted with methoxy, morpholino, or piperidino groups. All the ... Read more >>

ChemMedChem (ChemMedChem)
[2018, 13(7):725-735]

Cited: 1 time

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Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents.

Adnan A Bekhit, Ahmed M Farghaly, Ragab M Shafik, Mona M A Elsemary, Alaa El-Din A Bekhit, Aida A Guemei, Mai S El-Shoukrofy, Tamer M Ibrahim,

New thienopyrimidinone and triazolothienopyrimidinone derivatives have been synthesized. These compounds were subjected to anti-inflammatory and antimicrobial activity screening aiming to identify new candidates that have dual anti-inflammatory and antimicrobial activities. Compounds 5, 7 and 10a showed minimal ulcerogenic effect and high selectivity towards human recombinant COX-2 over COX-1 enzyme. Their ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2018, 77:38-46]

Cited: 0 times

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Keratin: dissolution, extraction and biomedical application.

Amin Shavandi, Tiago H Silva, Adnan A Bekhit, Alaa El-Din A Bekhit,

Keratinous materials such as wool, feathers and hooves are tough unique biological co-products that usually have high sulfur and protein contents. A high cystine content (7-13%) differentiates keratins from other structural proteins, such as collagen and elastin. Dissolution and extraction of keratin is a difficult process compared to other natural ... Read more >>

Biomater Sci (Biomaterials science)
[2017, 5(9):1699-1735]

Cited: 27 times

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Synthesis, evaluation and modeling of some triazolothienopyrimidinones as anti-inflammatory and antimicrobial agents.

Adnan A Bekhit, Ahmed M Farghaly, Ragab M Shafik, Mona Ma Elsemary, Mai S El-Shoukrofy, Alaa El-Din A Bekhit, Tamer M Ibrahim,

<h4>Aim</h4>New triazolotetrahydrobenzothienopyrimidinone derivatives were synthesized.<h4>Experimental</h4>Their structures were confirmed, and their anti-inflammatory, antimicrobial activities and ulcerogenic potentials were evaluated.<h4>Results</h4>Compounds 7a, 10a and 11a showed minimal ulcerogenic effect and high selectivity toward human recombinant COX-2 over COX-1 enzyme with IC<sub>50</sub> values of 1.39, 1.22 and 0.56 μM, respectively. Their docking outcome correlated ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2017, 9(9):881-897]

Cited: 3 times

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Study of antileishmanial activity of 2-aminobenzoyl amino acid hydrazides and their quinazoline derivatives.

Sherine Nabil Khattab, Nesreen Saied Haiba, Ahmed Mosaad Asal, Adnan A Bekhit, Aida A Guemei, Adel Amer, Ayman El-Faham,

A new small library of 2-aminobenzoyl amino acid hydrazide derivatives and quinazolinones derivatives was synthesized and fully characterized by IR, NMR, and elemental analysis. The activity of the prepared compounds on the growth of Leishmania aethiopica promastigotes was evaluated. 2-Benzoyl amino acid hydrazide showed higher inhibitory effect than the quinazoline ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2017, 27(4):918-921]

Cited: 3 times

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Compounds Containing Azole Scaffolds as Cyclooxygenase Inhibitors: A Review.

Hanan M A Ragab, Adnan A Bekhit, Sherif A F Rostom, Alaa El-Din A Bekhit,

There has been considerable interest in azole-containing compounds as promising antiinflammatory agents. Designed compounds with five-membered nitrogen-containing nuclei have demonstrated good anti-inflammatory activity, indicating their potential for the treatment of this highly irritating condition. Pyrazoles, have attracted much more attention than other azoles, however, reports on other azoles demonstrated that ... Read more >>

Curr Top Med Chem (Current topics in medicinal chemistry)
[2016, 16(30):3569-3581]

Cited: 2 times

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Synthesis and Preliminary Biological Evaluation of 1,3,5-Triazine Amino Acid Derivatives to Study Their MAO Inhibitors.

Sherine N Khattab, Hosam H Khalil, Adnan A Bekhit, Mohamed Mokbel Abd El-Rahman, Ayman El-Faham, Fernando Albericio,

Three series of 4,6-dimethoxy-, 4,6-dipiperidino- and 4,6-dimorpholino-1,3,5-triazin-2-yl) amino acid derivatives were synthesized and characterized. A preliminary study for their monoamine oxidase inhibitory activity showed that compounds 7, 18, and 25 had MAO-A inhibition activity comparable to that of the standard clorgyline, with apparently more selective inhibitory activity toward MAO-A than ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2015, 20(9):15976-15988]

Cited: 4 times

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