Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Alain Pompon"'
Publikováno v:
European Journal of Organic Chemistry. 2001:2129-2134
A glucuronide-based prodrug of paclitaxel (taxol®) has been synthesized for use in antibody-directed enzyme prodrug therapy (ADEPT). This three-component prodrug was obtained by coupling a glucuronyl derivative of N-methylamino 4-nitrophenol (10) to
Autor:
Jean Louis Imbach, M Shafiee, Christian Périgaud, P. Augustijns, Thierry Lioux, David Egron, G. Van den Mooter, S. Varray, A.-L. Villard, Renaat Kinget, Gilles Gosselin, S. Deferme, Anne-Marie Aubertin, Alain Pompon
Publikováno v:
Journal of Pharmaceutical Sciences. 90:448-463
The in vitro anti‐HIV activity, stability, and potential for oral absorption of a phosphotriester derivative of AZT (zidovudine; 3′‐azido‐2′,3′‐deoxythymidine) bearing a new esterase‐labile S ‐acyl‐2‐thioethyl (SATE) group as tr
Autor:
G. Valette, Pieter Annaert, P. Augustijns, Jean Louis Imbach, Alain Pompon, Gilles Gosselin, Renaat Kinget, Samira Benzaria, Lieve Naesens, Sigrid Hatse, E. De Clercq, G. Van den Mooter
Publikováno v:
Pharmaceutical Research. 15:239-245
Purpose. To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA.
Autor:
Alain Pompon, André Kirn, Christian Périgaud, Jean Louis Imbach, A-M Aubertin, N. Schlienger, Gilles Gosselin, Isabelle Lefebvre
Publikováno v:
Nucleosides and Nucleotides. 16:1321-1324
The synthesis, in vitro anti-HIV activity, and preliminary stability studies of several mononucleoside phosphorodithiolate derivatives incorporating a new kind of bio-labile phosphate-protection, namely 0-pivaloyl-2-oxyethyl, are reported. Our prelim
Autor:
Gilles Gosselin, Isabelle Lefebvre, Jean-Louis Imbach, Jean-Luc Girardet, Christian Périgaud, Anne-Marie Aubertin, André Kirn, Alain Pompon
Publikováno v:
Journal of Medicinal Chemistry. 38:3941-3950
The synthesis, in vitro anti-HIV-1 activity, and decomposition pathways of several mononucleoside phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) incorporating a new kind of carboxylate esterase-labile transient phosphate-protect
Synthesis, Decomposition Pathways and 'In Vitro' Evaluation of Bioreversible Phosphotriesters of Azt
Autor:
Christian Périgaud, Anne-Marie Aubertin, André Kirn, Alain Pompon, Isabelle Lefebvre, Gilles Gosselin, Jean-Luc Girardet, Jean-Louis Imbach
Publikováno v:
Nucleosides, Nucleotides and Nucleic Acids. 14:763-766
The synthesis, pharmacokinetic data and biological evaluation of a series of phosphotriesters containing S-acyl-2-thioethyl groups as enzyme-labile phosphate protecting groups and AZT as a model are described. A comparison of pharmacokinetic data and
Publikováno v:
Antiviral Chemistry and Chemotherapy. 5:91-98
Bis(pivaloyloxymethyl) azidothymidine 5′-monophosphate (piv2-AZTMP) was designed as a cell membrane-permeable precursor of AZTMP. We have reported previously that when incubated with CEM cells deficient in thymidine kinase, piv2-AZTMP gives rise to
Publikováno v:
Antisense Res Dev
Antisense Res Dev, 1994, 4 (1), pp.9-18
Antisense Res Dev, 1994, 4 (1), pp.9-18
International audience; Several studies have shown that alpha-oligonucleotides (alpha-ONs) are more resistant to degradation by nucleases than are beta-oligonucleotides (beta-ONs), but a few exceptions have been reported. The present work indicates t
Autor:
Christian Périgaud, Thierry Beltran, Gilles Gosselin, Jean-Louis Imbach, Alain Pompon, Anne-Marie Aubertin, David Egron, Isabelle Lefebvre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1775-1777
A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in TK
Autor:
I. Lefebvre, Nathalie Schlienger, Gilles Gosselin, Thierry Beltran, Jean-Louis Imbach, Anne-Marie Aubertin, Christian Périgaud, Alain Pompon
Publikováno v:
ChemInform. 30
MonoSATE aryl phosphotriesters of AZT are able to deliver intracellularly the corresponding 5'-mononucleotide. This process requires activation by an esterase followed by a phosphodiesterase. This finding opens the way to the design of new pronucleot