Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Amal Wahhab"'
Autor:
Ljubomir Isakovic, Oscar M. Saavedra, David B. Llewellyn, Stephen Claridge, Lijie Zhan, Naomy Bernstein, Arkadii Vaisburg, Nadine Elowe, Andrea J. Petschner, Jubrail Rahil, Norman Beaulieu, France Gauthier, A. Robert MacLeod, Daniel Delorme, Jeffrey M. Besterman, Amal Wahhab
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2742-2746
Potent SAH analogues with constrained homocysteine units have been designed and synthesized as inhibitors of human DNMT enzymes. The five membered (2S,4S)-4-mercaptopyrrolidine-2-carboxylic acid, in 1a, was a good replacement for homocysteine, while
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12b27b210b122378d7edc0e3a1d17925
https://doi.org/10.1016/j.bmcl.2009.03.132
https://doi.org/10.1016/j.bmcl.2009.03.132
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c33ea1411905c14a49c5e81eae5869a9
https://doi.org/10.1016/j.bmcl.2009.03.113
https://doi.org/10.1016/j.bmcl.2009.03.113
Autor:
Jeffrey M. Besterman, Amal Wahhab, Alain Ajamian, Martin Allan, Sylvain Lefebvre, Alina Nicolescu, Robert Deziel, Eric Therrien, Jacques Rodrigue, Sukhdev Manku, Jubrail Rahil, Andrea J. Petschner, Zuomei Li, Marielle Fournel, James Wang, Tim Guo, Natalie Nguyen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1866-1870
We have recently reported on a novel class of histone deacetylase (HDAC) inhibitors bearing a sulfamide group as the zinc-binding unit. Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their struc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6abf3fd06e2b54e9501d6b7a35258c02
https://doi.org/10.1016/j.bmcl.2009.02.075
https://doi.org/10.1016/j.bmcl.2009.02.075
Autor:
Sylvain Lefebvre, Silvana Leit, Alina Nicolescu, Marielle Fournel, Anthony Panetta, Jeffrey M. Besterman, Jubrail Rahil, Amal Wahhab, Anne-Marie Lemieux, Sukhdev Manku, Christiane R. Maroun, Yves Andre Chantigny, Theresa P. Yan, Robert Deziel, Zuomei Li, David Smil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:688-692
In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2(1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/II
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c439dcbe0834654fc9fdc20ebf48fd5
https://doi.org/10.1016/j.bmcl.2008.12.045
https://doi.org/10.1016/j.bmcl.2008.12.045
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c793d69f791b3bd653b579bbb81a8c8
https://doi.org/10.1016/j.bmcl.2008.04.009
https://doi.org/10.1016/j.bmcl.2008.04.009
Autor:
Amal Wahhab, Johann Leban
Publikováno v:
Tetrahedron Letters. 41:1487-1490
The solid phase synthesis of 6-methyl-1,3-disubstituted uracils by condensation of resin-bound unsymmetrically substituted ureas with diketene in acetic acid is described. Cleavage from the resin with TFA gave the above-mentioned compounds in good to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bba3d9e79686d494e35929cb68d359bb
https://doi.org/10.1016/s0040-4039(99)02349-7
https://doi.org/10.1016/s0040-4039(99)02349-7
Autor:
David B. Llewellyn, Amal Wahhab
Publikováno v:
Tetrahedron Letters. 50:3939-3941
An efficient method for the preparation of base-substituted S -adenosyl- dl -homocysteine analogues as well as of 2-chloro-N 6 -alkylated S -adenosyl- dl -homocysteine analogues is described. The method uses a convergent strategy that employs a commo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f05471429bfc1c13b78be204a8e6bd8c
https://doi.org/10.1016/j.tetlet.2009.04.076
https://doi.org/10.1016/j.tetlet.2009.04.076
Autor:
Amal Wahhab, Johann Leban
Publikováno v:
Tetrahedron Letters. 40:235-238
The solid phase synthesis of unsymmetrically substituted diamides from symmetric dicar☐ylic acids is described. The process was conducted following these steps: (1) preactivation of the dicar☐ylic acid with BOP, (2) addition to amine resin, (3) r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::41e34d00ce9c1cabbc202e53c26e217d
https://doi.org/10.1016/s0040-4039(98)02327-2
https://doi.org/10.1016/s0040-4039(98)02327-2
Publikováno v:
ChemInform. 22
Optically pure (S)-cyclopent-2-en-1-ol, (c 1.1, CHCl3), and (S)-3-methoxycyclopentene, (c 3.86, n-hexane), were prepared from ethyl (1R,2S)-2-hydroxycyclopentanecarboxylate, which is readily availa...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e97327276282e05c44eb9ca3a42e6b6d
https://doi.org/10.1002/chin.199108149
https://doi.org/10.1002/chin.199108149
Publikováno v:
ChemInform. 22
In the course of our studies on geochemical biomarkers we required a series of lupane standards. We report here an efficient synthesis of lupane (1) in three steps from betulin (3) in an overall yield of 47.2%. 17β(H)-28-Norlupane (2) was obtained i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3adf765a8af4072fd3fb3c7ad30513c0
https://doi.org/10.1002/chin.199132221
https://doi.org/10.1002/chin.199132221