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A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities
- 1.0363152 - ÚOCHB 2012 RIV FR eng J - Journal Article
Jansa, Petr - Baszczyňski, Ondřej - Dračínský, Martin - Votruba, Ivan - Zídek, Zdeněk - Bahador, G. - Stepan, G. - Cihlar, T. - Mackman, R. - Holý, Antonín - Janeba, Zlatko
A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities.
European Journal of Medicinal Chemistry. Roč. 46, č. 9 (2011), s. 3748-3754. ISSN 0223-5234. E-ISSN 1768-3254
R&D Projects: GA MV VG20102015046
Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50390703
Keywords : prodrugs * phosphonodiamides * bis-amidates * acyclic nucleoside phosphonates * GS-9219
Subject RIV: CC - Organic Chemistry
Impact factor: 3.346, year: 2011
A novel and efficient method for the one-pot synthesis of diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates, starting from free phosphonic acids or phosphonate diesters is reported. The methodology has been applied to the synthesis of the potent anticancer agent GS-9219, and symmetrical bis-amidates of other biologically active phosphonic acids.
Permanent Link: http://hdl.handle.net/11104/0199212
Number of the records: 1