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Publication
Featured researches published by Nancy Zhou.
Journal of Medicinal Chemistry | 2008
Nancy Zhou; Oscar Moradei; Stephane Raeppel; Silvana Leit; Sylvie Frechette; Frédéric Gaudette; Isabelle Paquin; Naomy Bernstein; Giliane Bouchain; Arkadii Vaisburg; Zhiyun Jin; Jeff Gillespie; James C. Wang; Marielle Fournel; Pu T. Yan; Marie-Claude Trachy-Bourget; Ann Kalita; Aihua Lu; Jubrail Rahil; A. Robert MacLeod; Zuomei Li; Jeffrey M. Besterman; Daniel Delorme
The design, synthesis, and biological evaluation of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide 8 (MGCD0103) is described. Compound 8 is an isotype-selective small molecule histone deacetylase (HDAC) inhibitor that selectively inhibits HDACs 1-3 and 11 at submicromolar concentrations in vitro. 8 blocks cancer cell proliferation and induces histone acetylation, p21 (cip/waf1) protein expression, cell-cycle arrest, and apoptosis. 8 is orally bioavailable, has significant antitumor activity in vivo, has entered clinical trials, and shows promise as an anticancer drug.
Bioorganic & Medicinal Chemistry Letters | 2009
Michael Mannion; Stephane Raeppel; Stephen William Claridge; Nancy Zhou; Oscar Mario Saavedra; Ljubomir Isakovic; Lijie Zhan; Frédéric Gaudette; Franck Raeppel; Robert Deziel; Normand Beaulieu; Hannah Nguyen; Ian Chute; Carole Beaulieu; Isabelle Dupont; Marie-France Robert; Sylvain Lefebvre; Marja Dubay; Jubrail Rahil; James C. Wang; Hélène Ste-Croix; A. Robert MacLeod; Jeffrey M. Besterman; Arkadii Vaisburg
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) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.
Bioorganic & Medicinal Chemistry Letters | 2009
Stephane Raeppel; Stephen William Claridge; Oscar Mario Saavedra; Frédéric Gaudette; Lijie Zhan; Michael Mannion; Nancy Zhou; Franck Raeppel; Marie-Claude Granger; Ljubomir Isakovic; Robert Deziel; Hannah Nguyen; Normand Beaulieu; Carole Beaulieu; Isabelle Dupont; Marie-France Robert; Sylvain Lefebvre; Marja Dubay; Jubrail Rahil; James C. Wang; Hélène Ste-Croix; A. Robert MacLeod; Jeffrey M. Besterman; Arkadii Vaisburg
A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-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) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.
Bioorganic & Medicinal Chemistry Letters | 2009
Oscar Mario Saavedra; Stephen William Claridge; Lijie Zhan; Franck Raeppel; Marie-Claude Granger; Stephane Raeppel; Michael Mannion; Frédéric Gaudette; Nancy Zhou; Ljubomir Isakovic; Naomy Bernstein; Robert Deziel; Hannah Nguyen; Normand Beaulieu; Carole Beaulieu; Isabelle Dupont; James C. Wang; A. Robert MacLeod; Jeffrey M. Besterman; Arkadii Vaisburg
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 xenograft models in mice in vivo.
Bioorganic & Medicinal Chemistry Letters | 2008
Sylvie Frechette; Silvana Leit; Soon Hyung Woo; Guillaume Lapointe; Guillaume Jeannotte; Oscar Moradei; Isabelle Paquin; Giliane Bouchain; Stephane Raeppel; Frédéric Gaudette; Nancy Zhou; Arkadii Vaisburg; Marielle Fournel; Pu Theresa Yan; Marie-Claude Trachy-Bourget; Ann Kalita; Marie-France Robert; Aihua Lu; Jubrail Rahil; A. Robert MacLeod; Jeffrey M. Besterman; Zuomei Li; Daniel Delorme
The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs is described. Some of these compounds were shown to inhibit HDAC1 with IC(50) values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21(WAF1/Cip1), and inhibit proliferation of human cancer cells. In addition, certain compounds of this class were active in several human tumor xenograft models in vivo.
Bioorganic & Medicinal Chemistry Letters | 2009
Stephane Raeppel; Nancy Zhou; Frédéric Gaudette; Silvana Leit; Isabelle Paquin; Guillaume Larouche; Oscar Moradei; Sylvie Frechette; Ljubomir Isakovic; Daniel Delorme; Marielle Fournel; Ann Kalita; Aihua Lu; Marie-Claude Trachy-Bourget; Pu Theresa Yan; Jianhong Liu; Jubrail Rahil; James C. Wang; Jeffrey M. Besterman; Koji Murakami; Zuomei Li; Arkadii Vaisburg
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 hyperacetylation of histones, cause expression of the tumor suppressor protein p21(WAF1/CIP1), and inhibit cellular proliferation. Lead molecule of the series, compound 25 is metabolically stable, possesses favorable pharmacokinetic characteristics and is orally active in vivo in different mouse tumor xenograft models.
Archive | 2006
Oscar Mario Saavedra; Stephen William Claridge; Lijie Zhan; Franck Raeppel; Arkadii Vaisburg; Stephane Raeppel; Robert Deziel; Michael Mannion; Nancy Zhou; Ljubomir Isakovic
Bioorganic & Medicinal Chemistry Letters | 2006
Oscar Moradei; Silvana Leit; Nancy Zhou; Sylvie Frechette; Isabelle Paquin; Stephane Raeppel; Frédéric Gaudette; Giliane Bouchain; Soon Hyung Woo; Arkadii Vaisburg; Marielle Fournel; Ann Kalita; Aihua Lu; Marie-Claude Trachy-Bourget; Pu T. Yan; Jianhong Liu; Zuomei Li; Jubrail Rahil; A. Robert MacLeod; Jeffrey M. Besterman; Daniel Delorme
Bioorganic & Medicinal Chemistry Letters | 2008
Isabelle Paquin; Stephane Raeppel; Silvana Leit; Frédéric Gaudette; Nancy Zhou; Oscar Moradei; Oscar Mario Saavedra; Naomy Bernstein; Franck Raeppel; Giliane Bouchain; Sylvie Frechette; Soon Hyung Woo; Arkadii Vaisburg; Marielle Fournel; Ann Kalita; Marie-France Robert; Aihua Lu; Marie-Claude Trachy-Bourget; Pu Theresa Yan; Jianhong Liu; Jubrail Rahil; A. Robert MacLeod; Jeffrey M. Besterman; Zuomei Li; Daniel Delorme
Bioorganic & Medicinal Chemistry Letters | 2007
Arkadii Vaisburg; Isabelle Paquin; Naomy Bernstein; Sylvie Frechette; Frédéric Gaudette; Silvana Leit; Oscar Moradei; Stephane Raeppel; Nancy Zhou; Giliane Bouchain; Soon Hyung Woo; Zhiyun Jin; Jeff Gillespie; James C. Wang; Marielle Fournel; Pu Theresa Yan; Marie-Claude Trachy-Bourget; Marie-France Robert; Aihua Lu; Jimmy Yuk; Jubrail Rahil; A. Robert MacLeod; Jeffrey M. Besterman; Zuomei Li; Daniel Delorme