Bioorg Med Chem Lett. 2010 Jul 15;20(14):4156-8. doi: 10.1016/j.bmcl.2010.05.058. Epub 2010 May 20.

Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.

Wallace MB, Adams ME, Kanouni T, Mol CD, Dougan DR, Feher VA, O'Connell SM, Shi L, Halkowycz P, Dong Q.

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Takeda San Diego, 10410 Science Center Drive, San Diego, CA 92121, United States. michael.wallace@takedasd.com

Abstract

A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties.

PMID:: 20621728; [PubMed - indexed for MEDLINE]

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One-pot multicomponent synthesis of diversely substituted 2-aminopyrroles. A short general synthesis of rigidins A, B, C, and D.
Frolova LV, Evdokimov NM, Hayden K, Malik I, Rogelj S, Kornienko A, Magedov IV. Org Lett. 2011 Mar 4; 13(5):1118-21. Epub 2011 Jan 26.

Structures reported by this article

Crystal Structure Of The Human Mitogen-Activated Protein Kinase Kinase 1 (Mek 1) In Complex With Ligand And Mgadp

PDB: 3MBL

Source: Homo sapiens

Method: X-Ray Diffraction

Resolution: 2.6 Å

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Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
Bioorg Med Chem Lett. 2010 Jul 15 ;20(14):4156-8. doi: 10.1016/j.bmcl.2010.05.058. Epub 2010 May 20 .

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