Browsing by Author "Motaleb M.A."

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Design, synthesis and biological evaluation of some novel sulfonamide derivatives as apoptosis inducers
(Elsevier Masson SAS, 2017) Mohamed K.O.; Nissan Y.M.; El-Malah A.A.; Ahmed W.A.; Ibrahim D.M.; Sakr T.M.; Motaleb M.A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; National Cancer Institute; Cancer Biology Department; Cairo University; Egypt; Faculty of Science; Cairo University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt
Several novel thiazolidinone and fused thiazolidinone derivatives bearing benzenesulfonamide moiety were synthesized and confirmed via spectral and elemental analyses. The newly synthesized compounds were evaluated for their cytotoxic activity on colorectal cancer cell line (Caco-2). All the synthesized compounds showed better activity than the reference standards (Doxorubicin and 5-FU). Investigation of the apoptotic activity of the most active compounds revealed that compounds 3a, 5a, 5c and 6c activate both caspase-3 and Fas-ligand in Caco-2�cell line. Compound 3a was the most active compound with caspase-3 concentration of 0.43�nmol/mL and Fas-ligand concentration of 775.2�pg/mL in treated Caco-2�cells. Compound 3a was radiolabeled with 99mTc and its biodistribution pattern was evaluated in�vivo using normal Swiss Albino mice. 99mTc-compound 3a complex didn't exhibit any accumulation in any body organs except for its accumulation in the colon; target organ; where it showed 8.97��1.35 %ID/g at 15min p. i. that elevated till 16.02��2.43 %ID/g at 120min p. i. � 2017 Elsevier Masson SAS
I-131 doping of silver nanoparticles platform for tumor theranosis guided drug delivery
(Elsevier B.V., 2018) Sakr T.M.; Khowessah O.M.; Motaleb M.A.; Abd El-Bary A.; El-Kolaly M.T.; Swidan M.M.; Radioactive Isotopes and Generator Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Modern Sciences and Arts University; 6th October City; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Cairo University; PO11562; Cairo; Egypt; Labeled Compounds Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt
Nanotechnology may be applied in medicine where the utilization of nanoparticles (?100 nm) for the delivery and targeting of theranostic agents is at the forefront of projects in cancer nano-science. This study points a novel one step synthesis approach to build up polyethylene glycol capped silver nanoparticles doped with I-131 radionuclide (131I-doped Ag-PEG NPs). The formula was prepared with average hydrodynamic size 21 nm, zeta potential � 25 mV, radiolabeling yield 98 � 0.76%, and showed good in-vitro stability in saline and mice serum. The in-vitro cytotoxicity study of cold Ag-PEG NPs formula as a drug carrier vehicle showed no cytotoxic effect on normal cells (WI-38 cells) at a concentration below 3 ?L/104 cells. The in-vivo biodistribution pattern of 131I-doped Ag-PEG NPs in solid tumor bearing mice showed high radioactivity accumulation in tumor tissues with maximum uptake of 35.43 � 1.12 and 63.8 � 1.3% ID/g at 60 and 15 min post intravenous (I.V.) and intratumoral injection (I.T.), respectively. Great potential of T/NT ratios were obtained throughout the experimental time points with maximum ratios 45.23 � 0.65 and 92.46 � 1.02 at 60 and 15 min post I.V. and I.T. injection, respectively. Thus, 131I-doped Ag-PEG NPs formulation could be displayed as a great potential tumor nano-sized theranostic probe. � 2018 Elsevier B.V.
Radiosynthesis, molecular modeling studies and biological evaluation of 99mTc-Ifosfamide complex as a novel probe for solid tumor imaging
(Taylor and Francis Ltd, 2018) Motaleb M.A.; El-Safoury D.M.; Abd-Alla W.H.; Awad G.A.S.; Sakr T.M.; Labelled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; College of Pharmaceutical Sciences and Drug Manufacturing; Misr University for Science & Technology; Giza; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Ain Shams University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt
Purpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. Materials and methods: The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 ?g of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. Results: A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3. 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ?3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. Conclusion: These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging. 2018, Copyright 2018 Taylor & Francis Group, LLC.