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

Theodor Bilharz Research Institute

Bibliographic Information

Authors: Mehany M.M.; Hammam O.A.; Selim A.A.; Sayed G.H.; Anwer K.E.

Journal: Scientific Reports

Publisher: Nature Research

Publication Date: 1 February 2024

Volume / Issue: Volume 14 / Issue 1

Article No.: 2738

ISSN: 20452322

DOI: 10.1038/s41598-024-53228-4

Scopus: View on Scopus

PubMed: 38302640

Document Type: Article

Access: All Open Access; Gold Open Access; Green Open Access

Authors and Affiliations

Mehany M.M., Laboratory Department, Chemistry Unit, Police Hospital, Agouza, Cairo, Egypt; Hammam O.A., Pathology Department, Theodor Bilharz Research Institute, Giza, Egypt; Selim A.A., Labeled Compounds Department, Hot Laboratories Centre, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt; Sayed G.H., Heterocyclic Synthesis Lab., Chemistry Department, Faculty of Science, Ain Shams University, Abbassia, Cairo, 11566, Egypt; Anwer K.E., Heterocyclic Synthesis Lab., Chemistry Department, Faculty of Science, Ain Shams University, Abbassia, Cairo, 11566, Egypt

Abstract

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. © 2024, The Author(s).

Keywords

Animals; Antineoplastic Agents; Caco-2 Cells; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Humans; Iodine Radioisotopes; MCF-7 Cells; Mice; Molecular Docking Simulation; Molecular Structure; Pyridines; Structure-Activity Relationship; antineoplastic agent; pyridine derivative; radioactive iodine; animal; Caco-2 cell line; chemical structure; chemistry; drug screening; human; MCF-7 cell line; molecular docking; mouse; structure activity relation

Citation Information

Scopus Citations: 28

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