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Article

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.

Journal of medicinal chemistry - 12 Aug 2010

Choi Hwan Geun, Ren Pingda, Adrian Francisco, Sun Fangxian, Lee Hyun Soo, Wang Xia, Ding Qiang, Zhang Guobao, Xie Yongping, Zhang Jianming, Liu Yi, Tuntland Tove, Warmuth Markus, Manley Paul W, Mestan Jürgen, Gray Nathanael S, Sim Taebo

Abstract excerpt

The second generation of Bcr-Abl inhibitors nilotinib, dasatinib, and bosutinib developed to override imatinib resistance are not active against the T315I "gatekeeper" mutation. Here we describe a type-II T315I inhibitor 2 (GNF-7), based upon a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffold which is capable of potently inhibiting wild-type and T315I Bcr-Abl as well as other clinically relevant Bcr-Abl...

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Identifiers

PMID: 20604564
DOI: 10.1021/jm901808w
PMCID: PMC4134510

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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