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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

SYSNO ASEP	0363152
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities
Author(s)	Jansa, Petr (UOCHB-X)_RID Baszczyňski, Ondřej (UOCHB-X)_{RID, ORCID} Dračínský, Martin (UOCHB-X)_{RID, ORCID} Votruba, Ivan (UOCHB-X)_RID Zídek, Zdeněk (UEM-P) Bahador, G. (US) Stepan, G. (US) Cihlar, T. (US) Mackman, R. (US) Holý, Antonín (UOCHB-X) Janeba, Zlatko (UOCHB-X)_{RID, ORCID}
Number of authors	11
Source Title	European Journal of Medicinal Chemistry. - : Elsevier - ISSN 0223-5234 Roč. 46, č. 9 (2011), s. 3748-3754
Number of pages	7 s.
Language	eng - English
Country	FR - France
Keywords	prodrugs ; phosphonodiamides ; bis-amidates ; acyclic nucleoside phosphonates ; GS-9219
Subject RIV	CC - Organic Chemistry
R&D Projects	VG20102015046 GA MV - Ministry of Interior (MV)
CEZ	AV0Z40550506 - UOCHB-X (2005-2011)
	AV0Z50390703 - UEM-P (2007-2013)
UT WOS	000295237400022
DOI	10.1016/j.ejmech.2011.05.040
Annotation	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.
Workplace	Institute of Organic Chemistry and Biochemistry
Contact	asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
Year of Publishing	2012

Number of the records: 1