Stéphane Raeppel scite author profile

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.

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Amphoteric Character of 2-Vinyloxiranes: Synthetic Equivalents ofβ,γ-Unsaturated Aldehydes and a Vinylogous Enolate

Lautens

Raeppel

2000

Angew. Chem. Int. Ed.

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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

Mannion

Raeppel

Claridge

et al. 2009

Bioorganic & Medicinal Chemistry Letters

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N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

Saavedra¹,

Claridge²,

Zhan³

et al. 2009

Bioorganic & Medicinal Chemistry Letters

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Identification of a novel series of potent RON receptor tyrosine kinase inhibitors

Raeppel

Gaudette

Mannion

et al. 2010

Bioorganic & Medicinal Chemistry Letters

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

Fréchette¹,

Leit²,

Woo³

et al. 2008

Bioorganic & Medicinal Chemistry Letters

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Lewis acid-catalyzed Mannich type reactions with potassium organotrifluoroborates

Tremblay-Morin¹,

Raeppel²,

Gaudette³

2004

Tetrahedron Letters

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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

Raeppel

Claridge

Saavedra

et al. 2009

Bioorganic & Medicinal Chemistry Letters

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