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

Abstract：

: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 (IC(50)=5-7 microM).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wittine K,Benci K,Rajić Z,Zorc B,Kralj M,Marjanović M,Pavelić K,De Clercq E,Andrei G,Snoeck R,Balzarini J,Mintas M

doi

10.1016/j.ejmech.2008.03.037

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

143-51

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00162-1

journal_volume

44

pub_type

杂志文章

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