Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Franck Raeppel"'
SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes
Autor:
Stephen William Claridge, Daniel Delorme, Ljubomir Isakovic, David B. Llewellyn, Franck Raeppel, A. Robert MacLeod, Jeffrey M. Besterman, Amal Wahhab, Norman Beaulieu, Arkadii Vaisburg, Lijie Zhan, Jubrail Rahil, Oscar Mario Saavedra, Nadine Elowe, Naomy Bernstein, Andrea J. Petschner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2747-2751
The inhibitory activity of base-modified SAH analogues and the specificity of inhibiting human DNMT1 and DNMT3b2 enzymes was explored. The 6-amino group was essential while the 7-N of the adenine ring of SAH could be replaced by CH- without loss of a
Autor:
Annie Barsalou, Normand Beaulieu, Marja Dubay, Naomy Bernstein, Jeff Gillespie, Marie-France Robert, Jubrail Rahil, Isabelle Dupont, Ian Chute, Sylvain Lefebvre, Marie-Claude Granger, Hannah Nguyen, Oscar Mario Saavedra, James Wang, Jeffrey M. Besterman, Serge Gravel, Amal Wahhab, Lijie Zhan, Arkadii Vaisburg, Roussen Pascal, Carole Beaulieu, Zhiyun Jin, Franck Raeppel, Robert Deziel, David B. Llewellyn, A. Robert MacLeod, Stephen William Claridge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2793-2798
A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC50 values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(18)
New heteroarylcarboxamide head groups substituted with two aromatic rings analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent inhibitors of RON tyrosine kinase with various level of selectivity for
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
New fused bicyclic lactam head groups as rigidified analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Depending on the functionalities and the size of these bicyclic head groups, potent inhibitors of RON
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(12)
New carboxamide head group analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent and selective inhibitors of RON enzyme versus c-Met RTK were obtained.
Publikováno v:
Tetrahedron Letters. 40:6377-6381
The perhydrobenz[ e ]indene moiety of the stellettins and of the stelliferins, two families of isomalabaricane-type triterpenes with trans-syn-trans ring junctions, has been built from a bicyclic γ,δ-unsaturated aldehyde by a reaction sequence incl
Autor:
Franck Raeppel, Denis Heissler
Publikováno v:
Synlett. :2534-2536
The difficult coupling of a geranyl- and an isocopalenyl moiety to form tricyclohexaprenol could be carried out by allylation of isocopalenal with an 8-geranylbarium chloride followed by reduction of the so-formed hindered hydroxy group via a xanthat
Publikováno v:
ChemInform. 29
Publikováno v:
Synlett. 2000:0874-0876
Autor:
Jeffrey M. Besterman, Naomy Bernstein, Hannah Nguyen, Franck Raeppel, Lijie Zhan, Stephane Raeppel, James Wang, A. Robert MacLeod, Marie-Claude Granger, Ljubomir Isakovic, Stephen William Claridge, Normand Beaulieu, Carole Beaulieu, Oscar Mario Saavedra, Frédéric Gaudette, Arkadii Vaisburg, Isabelle Dupont, Michael Mannion, Nancy Z. Zhou, Robert Deziel
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(24)
A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC(50) values in the low nanomolar range in vitro and were efficacious in human tumor xe