Browsing by Author "A Khedr, Mohammed"

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    99mTc-amitrole as a novel selective imaging probe for solid tumor: In silico and preclinical pharmacological study
    (Elsevier, 2015) Essa, BM; Sakr, TM; A Khedr, Mohammed; El-Essawy, FA; El-Mohty, AA
    Lactoperoxidase (LPO) inhibitors are very selective for solid tumor due to their high binding affinity to the LPO enzyme. A computational study was used to select top-ranked LPO inhibitor (alone and in complex with 99mTc) with high in silico affinity. The novel prepared 99mTc-amitrole complex demonstrated both in silico and in vivo high affinity toward solid tumors. 99mTc-amitrole was radio-synthesized with a high radiochemical yield (89.7 ± 3.25). It showed in vitro stability for up to 6 h. Its preclinical evaluation in solid tumor-bearing mice showed high retention and biological accumulation in solid tumor cells with a high Target/Non-Target (T/NT) ratio equal to 4.9 at 60 min post-injection. The data described previously could recommend 99mTc-amitrole as potential targeting scintigraphic probe for solid tumor imaging
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    Rational design of some substituted phenyl azanediyl (bis) methylene phosphonic acid derivatives as potential anticancer agents and imaging probes: Computational inputs, chemical synthesis, radiolabeling, biodistribution and gamma scintigraphy
    (ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) A Khedr, Mohammed; M Rashed, Hassan; Farag, Hamed; M Sakr, Tamer
    Bisphosphonates are widely used for treatment of osteoporosis. Recently, they have been reported to be effective anticancer agents. In this work, we designed some substituted phenyl (azanediyl) bis (methylene phosphonic acid) to be tested for their anticancer effect. Both molecular docking and dynamics studies were used to select the top ranked highly scored compounds. The selected hits showed potential in vitro anticancer effect against some cell lines. Biodistribution pattern and gamma scintigraphy were conducted to the most effective derivative (BMBP) after radiolabeling with 99mTc. Results of biodistribution and scintigraphic imaging of 99mTc-BMBP in tumor bearing mice showed a notable tumor affinity, and confirmed the targeting affinity of BMBP to the tumor tissues. As a conclusion, BMBP could act as potential anticancer agent and imaging probe