Bone targeted new zoledronate derivative: design, synthesis, <sup>99m</sup>Tc-coupling, <i>in-silico</i> study and preclinical evaluation for promising osteosarcoma therapy

Fayez, Hend; Selim, Adli A.

doi:10.1080/09553002.2022.2074162

Cited by 3 publications

(2 citation statements)

References 45 publications

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“…The radioactivity of each organ was counted using a NaI (Tl) crystal gamma counter. Bone, blood, and muscles were evaluated as 10, 7, and 40% of the body weight, respectively 54 . % Injected dose per gram (% ID/gram ± S.D.)…”

Section: Ethical Statementmentioning

confidence: 99%

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Mehany,

Hammam,

Selim

et al. 2024

Sci Rep

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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.

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Section: Ethical Statementmentioning

confidence: 99%

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Mehany,

Hammam,

Selim

et al. 2024

Sci Rep

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“…− was migrate at R f = 1.00 while colloid ([ 99m Tc]RH-Tc) and [ 99m Tc]Tc complex remained at R f = 0.00 [37,38].…”

Section: Pc (Paper Chromatography)mentioning

confidence: 99%

Synthesis, 99mTc-labeling, in-vivo study and in-silico investigation of 6-amino-5-[(bis-(2-hydroxy-ethyl)-amino]methyl]2-methyl pyrimidin-4-ol as a potential probe for tumor targeting

Essa

Abd‐Allah

Sakr

2022

J Radioanal Nucl Chem

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This study aimed to synthesize a new pyrimidine derivative with a good synthesis yield of 87% to act as a new cancer marker after radiolabeling with Tc-99m in a high radiochemical yield of 92.3%. In-vivo study in tumor-bearing Swiss albino mice model revealed promising data with high uptake in cancer. Docking study showed good binding interactions of the radiosynthesized complex at the binding site. In conclusion, this novel complex could be a potential probe for cancer targeting.

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Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning

Motaleb,

Ibrahim,

Shweeta

et al. 2024

Pharm Chem J

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Bone targeted new zoledronate derivative: design, synthesis, ^99mTc-coupling, in-silico study and preclinical evaluation for promising osteosarcoma therapy

Cited by 3 publications

References 45 publications

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Synthesis, 99mTc-labeling, in-vivo study and in-silico investigation of 6-amino-5-[(bis-(2-hydroxy-ethyl)-amino]methyl]2-methyl pyrimidin-4-ol as a potential probe for tumor targeting

Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning

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Bone targeted new zoledronate derivative: design, synthesis, 99mTc-coupling, in-silico study and preclinical evaluation for promising osteosarcoma therapy

Cited by 3 publications

References 45 publications

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments

Synthesis, 99mTc-labeling, in-vivo study and in-silico investigation of 6-amino-5-[(bis-(2-hydroxy-ethyl)-amino]methyl]2-methyl pyrimidin-4-ol as a potential probe for tumor targeting

Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning

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Bone targeted new zoledronate derivative: design, synthesis, ^99mTc-coupling, in-silico study and preclinical evaluation for promising osteosarcoma therapy