Tailoring Methotrexate for Precision Cancer Therapy: Synthesis, Characterization, and Anti-Cancer Profiling of Novel Analogues

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Rahul Subhash Buchade
Krishna Chandra Panda
Yasmin Khatoon
Touseef Begum
Vineet Joshi
Yogesh Baban Zambare
R senthilraj
Jisha Joseph


One of the most widely used chemotherapeutics is methotrexate, a structural counterpart of folic acid, which is particularly useful in haematological malignancies, different solid tumours, and inflammatory illnesses. Objective: Two methotrexate analogues have been synthesized in the current study and are being characterised and biologically assessed. Methods: To obtain the desired methotrexate analogues, a thoroughly examined and studied scheme was employed. The compounds were synthesised by a two-step process followed by a substitution reaction at the pteridine nucleus. The structures of analogues of Methotrexate were elucidated with spectral techniques viz. infrared, nuclear magnetic resonance and mass spectrometry. The antitumor efficacy of the produced compounds was assessed in HCC 1937 cells. Results: Using spectral methods, two successful analogues of methotrexate were synthesised and described. At various concentrations, the anticancer activity was assessed and contrasted with controls. Conclusion: The results indicated that both the analogues of Methotrexate demonstrated significant cell growth inhibition activity.

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