The novel phosphoramidate derivatives of NSAID 3-hydroxypropylamides: Synthesis, cytostatic and antiviral activity evaluations

The target phosphoramidates 5a–e were prepared in one step from 3-hydroxypropyl derivatives 3a–e of nonsteroidal anti-inflammatory drugs (fenoprofen, ketoprofen, ibuprofen, indomethacin, diclofenac). The products 3a–e and 5a–e were evaluated for their cytostatic and antiviral activity against malignant tumour cell lines and normal human fibroblasts (WI 38). All phosphoramidate derivatives 5a–e possess significantly greater inhibitory activities than the corresponding 3-hydroxypropyl derivatives 3a–e, whereby compound 5a showed the most potent inhibitory activities against cervical, pancreatic and colon carcinoma cell lines (IC50 = 5 − 7 μM).

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