Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance

GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo

(2016) Zhang Zhang et al.   CANCER LETTERS

Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-AblT315I mutant

(2015) Xiaoyun Lu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase

(2015) Xu Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of GZD824 as an Orally Bioavailable Inhibitor That Targets Phosphorylated and Nonphosphorylated Breakpoint Cluster Region–Abelson (Bcr-Abl) Kinase and Overcomes Clinically Acquired Mutation-Induced Resistance against Imatinib

(2013) Xiaomei Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Developments in the Third Generation Inhibitors of Bcr-Abl for Overriding T315I Mutation

(2012) X. Y. Lu et al.   CURRENT MEDICINAL CHEMISTRY

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

(2011) Wayne W. Chan et al.   CANCER CELL

New Opportunities to Treat the T315I-Bcr-Abl Mutant in Chronic Myeloid Leukaemia: Tyrosine Kinase Inhibitors and Molecules that Act by Alternative Mechanisms

(2010) S. Schenone et al.   CURRENT MEDICINAL CHEMISTRY

A Type-II Kinase Inhibitor Capable of Inhibiting the T315I “Gatekeeper” Mutant of Bcr-Abl

(2010) Hwan Geun Choi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

Imatinib and beyond—exploring the full potential of targeted therapy for CML

(2009) Alfonso Quintás-Cardama et al.   Nature Reviews Clinical Oncology

Molecular biology of bcr-abl1-positive chronic myeloid leukemia

(2008) A. Quintas-Cardama et al.   BLOOD

Inhibitors of ABL and the ABL-T315I Mutation

(2008) Glenn Noronha et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Abl tyrosine kinase inhibitors for overriding Bcr–Abl/T315I: from the second to third generation

(2008) Ruriko Tanaka et al.   Expert Review of Anticancer Therapy