Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Ljubomir Isakovic"'
Publikováno v:
Tetrahedron. 66:368-378
The application of a [6+4] cycloaddition strategy toward the synthesis of CP-225,917 is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3373d75be2ed75c966949402804b05a4
https://doi.org/10.1016/j.tet.2009.10.071
https://doi.org/10.1016/j.tet.2009.10.071
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:
James Wang, Pu Theresa Yan, Stephane Raeppel, Daniel Delorme, Oscar Moradei, Guillaume Larouche, Marielle Fournel, Jianhong Liu, Jeffrey M. Besterman, Frédéric Gaudette, Koji Murakami, Jubrail Rahil, Isabelle Paquin, Sylvie Frechette, Zuomei Li, Nancy Z. Zhou, Ann Kalita, Arkadii Vaisburg, Silvana Leit, Aihua Lu, Marie-Claude Trachy-Bourget, Ljubomir Isakovic
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:644-649
Analogues of the clinical compound MGCD0103 (A) were designed and synthesized. These compounds inhibit recombinant human HDAC1 with IC(50) values in the sub-micromolar range. In human cancer cells growing in culture these compounds induce hyperacetyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07246803c1a7f1f787b483907d478e2d
https://doi.org/10.1016/j.bmcl.2008.12.048
https://doi.org/10.1016/j.bmcl.2008.12.048
Publikováno v:
ChemInform. 33
The carbocyclic core of CP-225,917 and CP-263,114 is accessible through the [6+4] cycloaddition of a tropone with a 2-substituted cyclopentadiene. Examination of this reaction has revealed for the first time that this cycloaddition process is catalyz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::992b435e054d07a75cbacf060760c307
https://doi.org/10.1002/chin.200222086
https://doi.org/10.1002/chin.200222086
Autor:
Michael Mannion, James Wang, Jeffrey M. Besterman, Stephane Raeppel, Normand Beaulieu, Isabelle Dupont, Ljubomir Isakovic, Arkadii Vaisburg, Carole Beaulieu, Hannah Nguyen, Oscar Mario Saavedra, Robert Deziel, Christiane R. Maroun, A. Robert MacLeod, Stephen William Claridge, Frédéric Gaudette
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(9)
A novel series of N-(3-fluoro-4-(2-substituted-thieno[3,2-b]pyridin-7-yloxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamides targeting RON receptor tyrosine kinase was designed and synthesized. SAR study of the series allowed us to ide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a0704acb6cc44fac3645e2f914bbb95
https://pubmed.ncbi.nlm.nih.gov/20363625
https://pubmed.ncbi.nlm.nih.gov/20363625
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f64dc57acf05dac78df5d852f13dcfc5
https://pubmed.ncbi.nlm.nih.gov/19896842
https://pubmed.ncbi.nlm.nih.gov/19896842
Autor:
Carole Beaulieu, Marja Dubay, Jeffrey M. Besterman, Stephane Raeppel, Jubrail Rahil, Nancy Z. Zhou, Ian Chute, Arkadii Vaisburg, Lijie Zhan, Isabelle Dupont, Hannah Nguyen, Ljubomir Isakovic, James Wang, Robert Deziel, Stephen William Claridge, Frédéric Gaudette, A. Robert MacLeod, Normand Beaulieu, Hélène Ste-Croix, Marie-France Robert, Sylvain Lefebvre, Oscar Mario Saavedra, Michael Mannion, Franck Raeppel
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(23)
A series of N-(4-(6,7-disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC(50)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a9020f89c6b464506c2acebb912014e
https://pubmed.ncbi.nlm.nih.gov/19854051
https://pubmed.ncbi.nlm.nih.gov/19854051
Publikováno v:
Organic letters. 3(26)
The carbocyclic core of CP-225,917 and CP-263,114 is accessible through the [6+4] cycloaddition of a tropone with a 2-substituted cyclopentadiene. Examination of this reaction has revealed for the first time that this cycloaddition process is catalyz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4da56281b4d3ce36b3fb719cccb01df8
https://pubmed.ncbi.nlm.nih.gov/11784174
https://pubmed.ncbi.nlm.nih.gov/11784174