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Preparation of 3-Substituted-1-Isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET Kinase Inhibitors
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC. (Peter Diner)
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC.
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC.
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2012 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 55, no 10, 4872-4876 p.Article in journal (Refereed) Published
Abstract [en]

A series of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines have been designed, synthesized, and evaluated as RET protein kinase inhibitors. On the basis of docking results, a small library of pyrazolopyrimidine compounds with an extended hydrophobic side arm was synthesized. The most promising of the compounds (7a) displayed efficient inhibition in vitro and good selectivity when tested on a panel of kinases. Furthermore, 7a inhibited GDNF-induced RET phosphorylation of ERK1/2 in MCF-7 breast cancer cells at concentrations as low as 100 nM.

Place, publisher, year, edition, pages
2012. Vol. 55, no 10, 4872-4876 p.
National Category
Natural Sciences
Research subject
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-174622DOI: 10.1021/jm3003944OAI: oai:DiVA.org:uu-174622DiVA: diva2:527957
Available from: 2012-05-23 Created: 2012-05-23 Last updated: 2017-12-07Bibliographically approved

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Publisher's full texthttp://dx.doi.org/10.1021/jm3003944

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Dinér, Peter

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