Work

New pyrano-pyridine conjugates as potential anticancer agents: design, synthesis and computational studies

Year: 2024

Type: article

Abstract: Aim New pyrano[3,2-c]pyridine 4a-h, 5–8 and pyrano[2,3-d]pyrimidin 9a,b series were designed and chemically synthesized.Methodology Using the standard drug doxorubicin, the novel chemical entities have been assessed in vitro as potential anticancer prospects on cell lines from liver, breast, colon, and lung cancer along with examining their inhibitory behaviors upon both EGFR and VEGFR-2 kinases.Results & conclusion Compared to erlotinib (IC50 = 0.18 µM), compounds 8a and 8b demonstrated the highest anticancer activity with IC50 Values 0.23 and 0.15 µM, respectively). Further, derivative 8a illustrated encouraging inhibitory characteristics against EGFR and VEGFR-2 (IC50 = 1.21 and 2.65 μM, respectively). A computational study was used to estimate the physicochemical and pharmacokinetic properties to afford insightful information about the newly synthesized agents.

Source: Future Medicinal Chemistry

DOI: 10.1080/17568919.2024.2431475

Authors: Aladdin M. Srour, Eman S. Nossier, Najla A. Altwaijry, Safeya M. Mousa, Hanem M. Awad, Heba S. A. Elzahabi

Institutions: National Research Centre, Al-Azhar University, Academy of Scientific Research and Technology, Princess Nourah bint Abdulrahman University

Language: English

Topic: Synthesis and biological activity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Research Centre, Princess Nourah Bint Abdulrahman University