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Oscar Moradei

Explore the profile of Oscar Moradei including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 15
Citations 365
Followers 0
Related Specialties
Biochemistry
Chemistry
Oncology
Top 10 Co-Authors
Daniel Delorme
Jeffrey M Besterman
Arkadii Vaisburg
Marie-Claude Trachy-Bourget
Zuomei Li
Marielle Fournel
Silvana Leit
Sylvie Frechette
Ann Kalita
Giliane Bouchain
Published In
Bioorg Med Chem Lett
J Med Chem
Mol Cancer Ther
ACS Chem Biol
Curr Top Med Chem
Affiliations
Soon will be listed here.
Recent Articles
1.
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma
Drew A, Moradei O, Jacques S, Rioux N, Boriack-Sjodin A, Allain C, et al.
Sci Rep . 2017 Dec; 7(1):17993. PMID: 29269946
CARM1 is an arginine methyltransferase with diverse histone and non-histone substrates implicated in the regulation of cellular processes including transcriptional co-activation and RNA processing. CARM1 overexpression has been reported in...
2.
Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates
Boriack-Sjodin P, Jin L, Jacques S, Drew A, Sneeringer C, Scott M, et al.
ACS Chem Biol . 2015 Nov; 11(3):763-71. PMID: 26551522
Coactivator-associated arginine methyltransferase 1 (CARM1) is a protein arginine N-methyltransferase (PRMT) enzyme that has been implicated in a variety of cancers. CARM1 is known to methylate histone H3 and nonhistone...
3.
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound
Mitchell L, Drew A, Ribich S, Rioux N, Swinger K, Jacques S, et al.
ACS Med Chem Lett . 2015 Jun; 6(6):655-9. PMID: 26101569
A novel aryl pyrazole series of arginine methyltransferase inhibitors has been identified. Synthesis of analogues within this series yielded the first potent, selective, small molecule PRMT6 inhibitor tool compound, EPZ020411....
4.
SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103)
Raeppel S, Zhou N, Gaudette F, Leit S, Paquin I, Larouche G, et al.
Bioorg Med Chem Lett . 2008 Dec; 19(3):644-9. PMID: 19114304
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...
5.
Histone deacetylase inhibitors in cancer therapy: new compounds and clinical update of benzamide-type agents
Moradei O, Vaisburg A, Martell R
Curr Top Med Chem . 2008 Aug; 8(10):841-58. PMID: 18673170
Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic "histone code," thereby producing changes...
6.
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor
Zhou N, Moradei O, Raeppel S, Leit S, Frechette S, Gaudette F, et al.
J Med Chem . 2008 Jun; 51(14):4072-5. PMID: 18570366
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...
7.
MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo
Fournel M, Bonfils C, Hou Y, Yan P, Trachy-Bourget M, Kalita A, et al.
Mol Cancer Ther . 2008 Apr; 7(4):759-68. PMID: 18413790
Nonselective inhibitors of human histone deacetylases (HDAC) are known to have antitumor activity in mice in vivo, and several of them are under clinical investigation. The first of these, Vorinostat...
8.
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors
Frechette S, Leit S, Woo S, Lapointe G, Jeannotte G, Moradei O, et al.
Bioorg Med Chem Lett . 2008 Jan; 18(4):1502-6. PMID: 18207391
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...
9.
Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors
Paquin I, Raeppel S, Leit S, Gaudette F, Zhou N, Moradei O, et al.
Bioorg Med Chem Lett . 2007 Dec; 18(3):1067-71. PMID: 18160287
Inhibition of histone deacetylases (HDAC) is emerging as a new strategy in human cancer therapy. The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides is presented herein. From the...
10.
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors
Vaisburg A, Paquin I, Bernstein N, Frechette S, Gaudette F, Leit S, et al.
Bioorg Med Chem Lett . 2007 Nov; 17(24):6729-33. PMID: 17977726
A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides were designed and synthesized. These compounds were shown to inhibit recombinant human HDAC1 with IC(50) values in the sub-micromolar range. In human cancer cells growing in...