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research Publications

31. Pfaller, M. et al.
Activity of MGCD290, a Hos2 inhibitor, in combination with azole antifungals against opportunistic fungal pathogens
Journal of Clinical Microbiology, Dec 2009, p. 3797-3804

30. Gaudette, F. et al.
Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups
Bioorganic & Medicinal Chemistry Letters 20 (2010) 848-852

29. Saavedra, O. et al.
N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases
Bioorganic & Medicinal Chemistry Letters 19 (2009) 6836-6839

28. Therrien, E. et al.
1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM 1)
Bioorganic & Medicinal Chemistry Letters 19 (2009) 6725-6732

27. Mannion, M. et al.
N-(4-(6,7-disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 19 (2009) 6552-6556

26. Tessier, P. et al.
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 19 (2009) 5684-5688

25. Manku, S. et al.
Synthesis and evaluation of lysine derived sulfamides as histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 19 (2009) 1866-1870


24. Raeppel, S. et al.
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 19 (2009) 1323-1328

23. Raeppel, S. et al.
SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitors N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103)
Bioorganic & Medicinal Chemistry Letters 19 (2009) 644-649


22. Moradei, O. et al.

Histone deacetylase inhibitors in cancer therapy: new compounds and clinical update of benzamide-type agents

Current Topics in Med Chem, 2008, 8 (June 2008).

 

21. Paquin, I. et al.

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

Bioorganic & Medicinal Chemistry Letters, 18(2008), pp. 1067-1071.

 

20. Garcia-Manero, G. et al

Phase I study of the oral isotype-selective histone deacetylase inhibitors MGCD0103 in leukemia .

Blood, 2008 May 21.

 

19. Bonfils, C. et al.

Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay

Clinical Cancer Research, 2008: 14(11), June 1, 2008.

 

18. Claridge, S. et al.

Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases

Bioorganic & Medicinal Chemistry Letters, 18 (April 2008), pp. 2793-2798.

 

17. Fournel, M. et al.

MGCD0103 , a novel isotype-selective HDAC inhibitor, has broad spectrum antitumor activity in vitro and in vivo

Molecular Cancer Therapeutics, April 2008, Vol. 7, No. 4: pp. 759-768.

 

16. Fréchette, S. et al.

4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters, February 2008.

 

15. Vaisburg, A. et al.

N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters, 17 (2007), pp. 6729-6733.

 

14. Moradei, O. et al.

Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity

Journal of Medicinal Chemistry, October 2007.

 

13. Moradei, O. et al.

Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters, 16 (2006), pp. 4048-4052.

 

12, Moradei, O. et al.

Histone deacetylase inhibitors: Latest developments, trends and prospects

Current Topics in Med. Chem. – Anti-cancer Agents, 2005, p. 5.

 

11. Vaisburg, A. et al.

(2-amino-phenyl)-amides of ω-substituted alkanoic acids as new histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2004, 14, pp. 283-287.

 

10. Tremblay-Morin, J.-P. et al.

Lewis acid-catalyzed Mannich type reactions with potassium organotrifluoroborates

Tetrahedron Letters, 2004, 45, pp. 3471-3474.

 

9. Bouchain, G. and Delorme, D.

Novel hydroxamate and anilide derivatives as potent histone deacetylase inhibitors: synthesis and antiproliferative evaluation

Current Medicinal Chemistry, 2003, 10, 22, pp. 2359-2372.

 

8. Davis, A. et al.

Phase I and pharmacologic study of the human DNA methyltransferase antisense oligonucleotide MG98 given as a 21-day continuous infusion every 4 weeks

Investigational New Drugs, 203, 21, pp. 85-97.

 

7. Bouchain, G. et al.

Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.

J. Med. Chem., 2003, 46, pp. 820-830.

 

6. Robert, M.-F., et al.

DNMT1 is required to maintain CpG methylation and aberrant gene silencing in human cancer cells

Nature Genetics, 2003, 33, pp. 61-65.

 

5. Reid, G. et al.

Selective inhibition of DNA methyltransferase enzymes as a novel strategy for cancer treatment

Current Opinion in Molecular Therapeutics, 2002, 4(2).

 

4. Woo, S. H. et al.

Structurally simple trichostatin a-like straight chain hydroxamates as potent histone deacetylase inhibitors

J. Med. Chem. 2002, 45, pp. 2877-2885.

 

3. Beaulieu, N. et al.

An essential role for DNA methyltransferase DNMT3B in cancer cell survival

J. Biol. Chem. 2002, 277, pp. 28176-28181.

 

2. Fournel. M. et al.

Sulfonamide anilides, a novel class of histone deacetylase inhibitors, are antiproliferative against human tumors

Cancer Research, 2002, 62, pp. 4325-4330.


1. 
Lavoie, R. et al.

Design and synthesis of a novel class of histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters, 11 (2001), pp. 2847-2850.

 








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