Ecofriendly Synthesis of New Azo Compounds as Antibacterial Agents: In Vitro Screening and Preliminary In Vivo Evaluation Using 131I-Radiolabeling Kurls E. Anwer, Basma M. Essa, Adli A. Selim, Galal H. Sayed, Safaa S. Shaban Archiv Der Pharmazie, 2026 This work is designed to establish sustainable routes for the synthesis of new variable azo heterocyclic derivatives via the reaction of 2‐[(dicyanomethyl)diazinyl]benzoic acid 2 with different nucleophilic agents, including hydrazine derivatives (such as phenyl hydrazine and 2,4‐dinitrophenylhydrazine), acylhydrazines (e.g., benzoylhydrazine), nitrogen‐based nucleophiles (semicarbazide and thiosemicarbazide), oxygen‐containing reagents (hydroxylamine), as well as urea, thiourea, guanidine hydrochloride, and o ‐phenylenediamine. Both conventional heating and microwave approaches were used to furnish the desired heterocycles. The compounds exhibited potent antibacterial activity against Gram‐positive and Gram‐negative pathogens, outperforming fluconazole. The lead compound was successfully radiolabeled with 131 I in high yield (87.72% RCY). In vivo evaluation in an infection model demonstrated excellent pharmacokinetics, with specific uptake in infected tissue (13.7% ID/g at 1 h) and a high target‐to‐non‐target ratio (6.31). These findings underscore the theranostic potential of these azo compounds, positioning them as both antimicrobial agents and candidate radiotherapeutics for infection.
99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting Adli A. Selim, Tamer M. Sakr, Basma M. Essa, Galal H. Sayed, Kurls E. Anwer Scientific Reports, 2025 Sulfonamide derivatives are a significant class of medicinal compounds. Gold nanoparticles (AuNPs) offer precise cancer treatment through targeted delivery, boasting high drug-loading capacity and low toxicity. This study aimed to develop and evaluate 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as a tumor-targeting agent. A novel benzenesulfonamide derivative bearing a pyridine moiety was synthesized. Compound 3 (4-((3-cyano-4-(2,4-dichlorophenyl)-6-phenylpyridin-2-yl)amino)-N-(diaminomethylene)benzenesulfonamide) exhibited remarkable anti-cancer activity against MCF-7 cells. The chemical reduction method was employed to create compound 3-citrate-AuNPs. A comprehensive examination of the synthesized nano-platform was conducted, including zeta potential, size analysis, radiochemical yield, and in-vivo biodistribution in tumor-bearing mice. The nano-platform was successfully produced with good stability, optimal particle size (9 nm diameter for AuNPs), and high radiochemical purity for [99mTc]Tc-compound 3 (88.31 ± 2.14%). In-vivo investigations revealed that intravenously administered [99mTc]Tc-compound 3-citrate-AuNPs accumulated in tumors with a high target-to-non-target ratio. The findings validate the efficacy of the novel [99mTc]Tc-compound 3-citrate-AuNPs platform as a tumor-targeting agent.
Actinium-225/Bismuth-213 as Potential Leaders for Targeted Alpha Therapy: Current Supply, Application Barriers, and Future Prospects Mohamed F. Nawar, Adli A. Selim, Basma M. Essa, Alaa F. El-Daoushy, Mohamed M. Swidan, et al. Cancers, 2025 Alpha therapy (TAT) relies on combining alpha-emitting radionuclides with specific cell-targeting vectors to deliver a high payload of cytotoxic radiation capable of destroying tumor tissues. TAT efficacy comes from the tissue selectivity of the targeting vector, the high linear energy transfer (LET) of the radionuclide, and the short range of alpha particles in tissues. Recent research studies have been directed to evaluate TAT on a preclinical and clinical scale, including evaluating damage to tumor tissues with minimal toxic radiation effects on surrounding healthy tissues. This review highlights the use of Actinium-225/Bismuth-213 radionuclides as promising candidates for TAT. Herein, we begin with a discussion on the production and supply of [225Ac]Ac/[213Bi]Bi followed by the formulation of [225Ac]Ac/[213Bi]Bi-radiopharmaceuticals using different radiolabeling techniques. Finally, we have summarized the preclinical and clinical evaluation of these potential radiotheranostic agents.
Silybin loaded Ag-nanoparticles as a drug delivery system for solid tumor theragnosis: Extraction, radioiodination, and biodistribution study Basma M. Essa, Islam M. Abdelmonem, Mohamed A. Amin, Adli A. Selim Archiv Der Pharmazie, 2025 Biocompatible silver nanoparticles (AgNPs) are employed with an active ingredient of milk thistle extract, silybin (SIB), to treat cancers. Strong cytotoxic effects of SIB‐AgNPs against two distinct cell lines (MCF‐7 and HepG2) are observed on a stable nano‐platform that contains spherical nanoparticles within a limited size range. With a high radiochemical purity, radioiodination of SIB‐AgNPs was accomplished. The investigation on the biodistribution of [131I]iodo‐SIB‐AgNPs in mice‐bearing tumors showed that SIB‐AgNPs prefer localization in tumor tissue. In conclusion, this work strengthens the case for [131I]iodo‐SIB‐AgNPs as an effective theranostic agent for tumor imaging and treatment.
Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments Marwa M. Mehany, Olfat A. Hammam, Adli A. Selim, Galal H. Sayed, Kurls E. Anwer Scientific Reports, 2024 Pyridine compounds are one of the most important heterocyclic derivatives showing wide ranges in biological and pharmacological activities. Green chemistry eliminates or reduces the generation of hazardous compounds. It prevents pollution at a molecular level. The microwave technique used in heterocyclic compound synthesis is also an important branch of green chemistry techniques. In this study, we report designing and synthesizing a new pyridine-bearing pentose moiety via a one-pot multicomponent reaction using D-glucose and also investigate its behavior and reactivity toward some simple and heterocyclic amino derivatives. The chemical structures of the synthesized compounds were characterized and tested for their cytotoxic activities. Some of the test compounds exhibited slight to high cytotoxic activities against Caco2 (colon cancer) cells, HepG2 (hepatocellular carcinoma) cells and MCF-7 (human breast cancer) cells by MTT assay. The results showed clearly that compound 4 and compound 8 displayed strongest to moderate cytotoxic activity against the HepG2, Caco2 and MCF-7 respectively and compound 1 showed good activity against MCF-7 in comparison to the standard anticancer drug doxorubicin. These data were by cytopathological examination. An in-vivo radioactive tracing study of compound 4 proved its targeting ability to sarcoma cells in a tumor-bearing mice model. Our findings suggest that the synthesized compounds may be promising candidates as novel anticancer agents.
Design, eco-friendly synthesis, antibacterial evaluation, radiolabeling and biodistribution study of some novel enaminonitrile pyridine derivatives KE Anwer, G Abdelaziz, BM Essa, AA Selim, AA El‐Sayed, ... Applied Radiation and Isotopes, 112608 , 2026 2026
Ecofriendly Synthesis of New Azo Compounds as Antibacterial Agents: In Vitro Screening and Preliminary In Vivo Evaluation Using 131 I‐Radiolabeling KE Anwer, BM Essa, AA Selim, GH Sayed, SS Shaban Archiv der Pharmazie 359 (4), e70245 , 2026 2026
Innovative Hybrid 99mTc-Exemestane Magnesium Nanoparticles: Pioneering Dual-Mode Theranostic and Precision Tumor Targeting AA Selim, MA Amin, MM Abouhashim, AB Ibrahim Journal of Drug Delivery Science and Technology, 107916 , 2025 2025 Citations: 1
Eco-friendly synthesis of novel enaminonitrile pyridine derivatives: 131 I-radiosynthesis, anticancer investigation and in vivo study in tumour-bearing mice AA Selim, BM Essa, SS Shaban, GH Sayed, MM Mehany, KE Anwer Journal of Drug Targeting, 1-9 , 2025 2025
Actinium-225/Bismuth-213 as Potential Leaders for Targeted Alpha Therapy: Current Supply, Application Barriers, and Future Prospects MF Nawar, AA Selim, BM Essa, AF El-Daoushy, MM Swidan, ... Cancers 17 (18), 3055 , 2025 2025 Citations: 4
Silybin loaded Ag‐nanoparticles as a drug delivery system for solid tumor theragnosis: Extraction, radioiodination, and biodistribution study BM Essa, IM Abdelmonem, MA Amin, AA Selim Archiv der Pharmazie 358 (3), e2400725 , 2025 2025 Citations: 4
99m Tc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting AA Selim, TM Sakr, BM Essa, GH Sayed, KE Anwer Scientific Reports 15 (1), 4687 , 2025 2025 Citations: 5
Revitalizing itraconazole: unleashing its anticancer potential through oral nanosystems for liver targeting and biodistribution profiling in an animal model using radiolabeling … E Abdelhakeem, AA Nemr, HM Rashed, AA Selim, BM Essa, D Hegazy Journal of Drug Delivery Science and Technology 104, 106463 , 2025 2025 Citations: 21
Synthesis and radiolabelled evaluation of novel pyrimidine derivatives as dual α-amylase inhibitors and GIT-targeted molecular imaging probe DA Elsayed, W Shehta, S El-Kalyoubi, A Selim, MG Assy, O Metwally, ... RSC advances 15 (36), 29544-29559 , 2025 2025 Citations: 4
Intranasal radioiodinated ferulic acid polymeric micelles as the first nuclear medicine imaging probe for ETRA brain receptor H Fayez, A Selim, R Shamma, H Rashed Current Radiopharmaceuticals 17 (2), 209-217 , 2024 2024 Citations: 4
Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments MM Mehany, OA Hammam, AA Selim, GH Sayed, KE Anwer Scientific Reports 14 (1), 2738 , 2024 2024 Citations: 30
Biogenic harmony of biocompatible silver nanoplatforms using chamomile extract and apigenin-7-glucoside for solid tumor therapy AA Selim, IM Abdelmonem, MA Amin, BM Essa Journal of Radioanalytical and Nuclear Chemistry 333 (2), 705-715 , 2024 2024 Citations: 5
Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique MA Shewaiter, AA Selim, HM Rashed, YM Moustafa, S Gad Journal of Cancer Research and Clinical Oncology 149 (20), 18065-18080 , 2023 2023 Citations: 11
Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo … E Taha, SA Nour, W Mamdouh, AA Selim, MM Swidan, AB Ibrahim, ... International Journal of Pharmaceutics: X 5, 100160 , 2023 2023 Citations: 48
Green synthesis of highly functionalized heterocyclic bearing pyrazole moiety for cancer-targeted chemo/radioisotope therapy KE Anwer, GH Sayed, BM Essa, AA Selim BMC chemistry 17 (1), 139 , 2023 2023 Citations: 16
Gold Nanoparticles: Synthesis, Functionalization and Biomedical Applications Especially in Cardiovascular Therapy AA Selim, TM Sakr, BM Essa Pharmaceutical Chemistry Journal 57 (1), 29-39 , 2023 2023 Citations: 10
Niosomes as a novel pharmaceutical carrier: structure, classification and preparation methods MA Mahmoud Records of Pharmaceutical and Biomedical Sciences 7 (3), 15-24 , 2023 2023 Citations: 8
Nanoemulsion formulation of pregabalin for enhanced nose to brain delivery and biological tracking using radiolabeling with 99mTc H Fayez, AA Selim, RN Shamma, HM Rashed Bulletin of Faculty of Pharmacy Cairo University 61 (1), 10 , 2023 2023 Citations: 1
New 5-aryl-1, 3, 4-thiadiazole-based anticancer agents: Design, synthesis, in vitro biological evaluation and in vivo radioactive tracing studies RM El-Masry, BM Essa, AA Selim, SZ El-Emam, KO Mohamed, TM Sakr, ... Pharmaceuticals 15 (12), 1476 , 2022 2022 Citations: 10
Radioiodinated acemetacin loaded niosomes as a dual anticancer therapy MA Shewaiter, AA Selim, YM Moustafa, S Gad, HM Rashed International Journal of Pharmaceutics 628, 122345 , 2022 2022 Citations: 20
MOST CITED SCHOLAR PUBLICATIONS
An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging MA Motaleb, ASA Adli, M El‐Tawoosy, MH Sanad, M AbdAllah Journal of Labelled Compounds and Radiopharmaceuticals 59 (4), 157-163 , 2016 2016 Citations: 58
Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo … E Taha, SA Nour, W Mamdouh, AA Selim, MM Swidan, AB Ibrahim, ... International Journal of Pharmaceutics: X 5, 100160 , 2023 2023 Citations: 48
Novel thiobarbiturates as potent urease inhibitors with potential antibacterial activity: Design, synthesis, radiolabeling and biodistribution study HG Abdulwahab, MF Harras, NG El Menofy, AM Hegab, BM Essa, ... Bioorganic & Medicinal Chemistry 28 (23), 115759 , 2020 2020 Citations: 45
Synthesis, radiolabeling and biological distribution of a new dioxime derivative as a potential tumor imaging agent MA Motaleb, AA Selim, M El-Tawoosy, MH Sanad, MA El-Hashash Journal of Radioanalytical and Nuclear Chemistry 314 (3), 1517-1522 , 2017 2017 Citations: 45
Synergistic cytotoxicity of shikonin‐silver nanoparticles as an opportunity for lung cancer H Fayez, MA El‐Motaleb, AA Selim Journal of Labelled Compounds and Radiopharmaceuticals 63 (1), 25-32 , 2020 2020 Citations: 44
Synthesis, characterization, radiolabeling and biodistribution of a novel cyclohexane dioxime derivative as a potential candidate for tumor imaging EHMA Motaleb MA, Selim AA, El-Tawoosy M, Sanad MH International Journal of Radiation Biology , 2018 2018 Citations: 43
Dioximes: Synthesis and biomedical applications MA Motaleb, AA Selim Bioorganic Chemistry 82, 145-155 , 2019 2019 Citations: 40
Platelet-12 lipoxygenase targeting via a newly synthesized curcumin derivative radiolabeled with technetium-99m RI Al-Wabli, TMMH Sakr, MA Khedr, AA Selim, MAEMA El-Rahman, ... Chemistry Central Journal 10 (1), 73 , 2016 2016 Citations: 39
Conventional and microwave-assisted synthesis, anticancer evaluation, 99mTc-coupling and In-vivo study of some novel pyrazolone derivatives BM Essa, AA Selim, GH Sayed, KE Anwer Bioorganic Chemistry 125, 105846 , 2022 2022 Citations: 36
Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments MM Mehany, OA Hammam, AA Selim, GH Sayed, KE Anwer Scientific Reports 14 (1), 2738 , 2024 2024 Citations: 30
Synthesis, characterization, and radiolabeling of heterocyclic bisphosphonate derivative as a potential agent for bone imaging MA Motaleb, MH Sanad, AA Selim, M El-Tawoosy, M Abd-Allah Radiochemistry 60 (2), 201-207 , 2018 2018 Citations: 30
Histopathology, pharmacokinetics and estimation of interleukin-6 levels of Moringa oleifera leaves extract-functionalized selenium nanoparticles against rats induced … KEAAAS Eman M. M. Ebrahem, Galal H. Sayed, Gehan N. A. Gad Cancer Nanotechnology 13 (14) , 2022 2022 Citations: 23
Revitalizing itraconazole: unleashing its anticancer potential through oral nanosystems for liver targeting and biodistribution profiling in an animal model using radiolabeling … E Abdelhakeem, AA Nemr, HM Rashed, AA Selim, BM Essa, D Hegazy Journal of Drug Delivery Science and Technology 104, 106463 , 2025 2025 Citations: 21
Radioiodinated acemetacin loaded niosomes as a dual anticancer therapy MA Shewaiter, AA Selim, YM Moustafa, S Gad, HM Rashed International Journal of Pharmaceutics 628, 122345 , 2022 2022 Citations: 20
Extraction, purification and radioiodination of Khellin as cancer theranostic agent AA Selim, BM Essa, IM Abdelmonem, MA Amin, MO Sarhan Applied Radiation and Isotopes 178, 109970 , 2021 2021 Citations: 18
Green synthesis of highly functionalized heterocyclic bearing pyrazole moiety for cancer-targeted chemo/radioisotope therapy KE Anwer, GH Sayed, BM Essa, AA Selim BMC chemistry 17 (1), 139 , 2023 2023 Citations: 16
Anti-cancer, anti-inflammatory and antioxidant effects of Vit-A/C@ SeNPs in mutual diethylnitrosamine and carbon tetrachloride induced hepatocellular damage in albino rats SA Aljuhr, G Abdelaziz, AA Selim, WA Zaghary, TM Sakr Journal of Drug Delivery Science and Technology 75, 103723 , 2022 2022 Citations: 13
Lung Cancer-Targeted [ 131 I]-Iodoshikonin as Theranostic Agent: Radiolabeling, In Vivo Pharmacokinetics and Biodistribution AA Selim, MA Motaleb, HA Fayez Pharmaceutical Chemistry Journal 55 (11), 1163-1168 , 2022 2022 Citations: 13
Preparation and preliminary evaluation study of [ 131 I]iodocolchicine-gallic-AuNPs: a potential scintigraphic agent for inflammation detection BM Essa, AA Selim, OA El-Kawy, G Abdelaziz International journal of radiation biology 98 (8), 1358-1365 , 2022 2022 Citations: 12
Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique MA Shewaiter, AA Selim, HM Rashed, YM Moustafa, S Gad Journal of Cancer Research and Clinical Oncology 149 (20), 18065-18080 , 2023 2023 Citations: 11