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Use of Pd-catalyzed Suzuki-Miyaura coupling reaction in the rapid synthesis of 5-aryl-6-(phosphonomethoxy)uracils and evaluation of their inhibitory potency on human thymidine phosphorylase
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SYSNO ASEP 0347416 Document Type C - Proceedings Paper (int. conf.) R&D Document Type The record was not marked in the RIV Title Use of Pd-catalyzed Suzuki-Miyaura coupling reaction in the rapid synthesis of 5-aryl-6-(phosphonomethoxy)uracils and evaluation of their inhibitory potency on human thymidine phosphorylase Author(s) Pomeisl, Karel (UOCHB-X) RID
Votruba, Ivan (UOCHB-X) RID
Horská, Květoslava (UOCHB-X)
Holý, Antonín (UOCHB-X)
Pohl, Radek (UOCHB-X) RID, ORCIDNumber of authors 5 Source Title International Roundtable on Nucleosides, Nucleotides and Nucleic Acids. IRT 2010. - Lyon : University of Lyon, 2010 Pages s. 86-87 Number of pages 2 s. Action International Roundtable on Nucleosides, Nucleotides and Nucleic Acids. IRT 2010 Event date 29.08.2010-03.09.2010 VEvent location Lyon Country FR - France Event type EUR Language eng - English Country FR - France Keywords ANPs ; human thymidine phosphorylase Subject RIV CC - Organic Chemistry R&D Projects 1M0508 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z40550506 - UOCHB-X (2005-2011) Annotation A number of new 5-aryl substituted pyrimidine acyclic nucleoside phosphonates were synthesized and tested for their ability to inhibit human TP. Their rapid synthesis using Pd-catalyzed Suzuki-Miyaura coupling reactions of various arylboronic acids with 5-bromo-4-(phosphonomethoxy)-2,6-dibutoxypyrimidine was succesfully applied. For a series of 5-aryl-6-phosphonomethoxyuracils, an increased multisubstrate inhibitory effect was determined. This effect is supported by the results found for 4-fluorophenyl and 3-nitrophenyl substituents. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2011
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