Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

doi:10.1021/jm2009925

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Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Journal of medicinal chemistry - 9 Feb 2012

Rowbottom Martin W, Faraoni Raffaella, Chao Qi, Campbell Brian T, Lai Andiliy G, Setti Eduardo, Ezawa Maiko, Sprankle Kelly G, Abraham Sunny, Tran Lan, Struss Brian, Gibney Michael, Armstrong Robert C, Gunawardane Ruwanthi N, Nepomuceno Ronald R, Valenta Ianina, Hua Helen, Gardner Michael F, Cramer Merryl D, Gitnick Dana, Insko Darren E, Apuy Julius L, Jones-Bolin Susan, Ghose Arup K, Herbertz Torsten, Ator Mark A, Dorsey Bruce D, Ruggeri Bruce, Williams Michael, Bhagwat Shripad, James Joyce, Holladay Mark W

Abstract excerpt

The Ras/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway plays a central role in the regulation of cell growth, differentiation, and survival. Expression of mutant BRAF(V600E) results in constitutive activation of the MAPK pathway, which can lead to uncontrolled cellular growth. Herein, we describe an SAR optimization campaign around a series of quinazoline derived BRAF(V600E) inhibitors. In...

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PMID: 22168626
DOI: 10.1021/jm2009925

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BRAF
BID

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