مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Information Journal Paper

Title

1, 3, 5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics

Pages

  295-301

Keywords

1 
3 

Abstract

 Objective(s): Osteosarcoma is a major solid malignant tumor of bone, possessing significant burden on healthcare due to non-availability of specific anticancer agents. The current study was conducted to identify novel 1, 3, 5-triazine derivatives against osteosarcoma. Materials and Methods: The compounds were synthesized in a straight-forward two-step reaction and subsequently tested against PI3K and mTOR kinase and anticancer activity against osteosarcoma cells (MG-63, U2-OS, and Saos-2). The effect of the most potent compound was evaluated on apoptosis and cell phase of Saos-2 cells. The pharmacological activity was further established in the patient-derived orthotopic xenograft (PDOX) mouse model. Results: The developed compounds 8 (a-f) showed significant inhibitory activities against PI3K, mTOR, and OS cells. Among the tested series, compound 8a showed highly potent PI3K/mTOR inhibitory activity with significant anticancer activity against Saos-2 cells compared with Imatinib as standard. It also induces apoptosis and causes G2/M arrest in Saos-2 cells. Compound 8a significantly improved body weight, reduced tumor volume, and inhibited lung metastasis in athymic nude mice in a PDOX mouse model. It also showed optimal pharmacokinetic parameters in SD rats. Conclusion: In summary, 1, 3, 5-triazine analogs were identified as new PI3K/mTOR inhibitors against osteosarcoma.

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    APA: Copy

    SU, QING, Xu, Baolin, Tian, Zhoubin, & Gong, Ziling. (2022). 1, 3, 5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 25(3), 295-301. SID. https://sid.ir/paper/991429/en

    Vancouver: Copy

    SU QING, Xu Baolin, Tian Zhoubin, Gong Ziling. 1, 3, 5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2022;25(3):295-301. Available from: https://sid.ir/paper/991429/en

    IEEE: Copy

    QING SU, Baolin Xu, Zhoubin Tian, and Ziling Gong, “1, 3, 5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 25, no. 3, pp. 295–301, 2022, [Online]. Available: https://sid.ir/paper/991429/en

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