Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.

Publication

Citation
Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H.: Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. J Med Chem, Volume 54 (7), 2011
Authors
Arzeno H, Bingenheimer W, Chen J, Dalrymple SA, Dewdney N, Dunn J, Farrell R, Frauchiger S, Gabriel T, Ghate M, Goldstein DM, Graves B, Hill RJ, Kuglstatter A, La Fargue J, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Sjogren EB, Soth M, Stahl M, Sung ML, Suttman RT, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H.
Journal
J Med Chem
Year
2011
PubMed
21375264
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Palacky University Olomouc

Palacky University Olomouc

Faculty of Science

Department of Physical Chemistry

tř. 17. listopadu 1192/12

771 46 Olomouc

Czech Republic

How to cite?

Juračka J., Šrejber M., Melíková M., Bazgier V., Berka K.: MolMeDB: Molecules on Membranes Database. Database, Volume 2019, 2019, baz078, https://doi.org/10.1093/database/baz078

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