Abl kinases are prototypic cytoplasmic tyrosine kinases and are involved in a variety of
chromosomal aberrations in different cancers. This causes the expression of Abl fusion …

Beginning with imatinib a decade ago, therapy based on targeted inhibition of the BCR-ABL
kinase has greatly improved the prognosis for chronic myeloid leukemia (CML) patients. The …

Transformations of aromatic compounds into the corresponding amines, amides, and imides
through carbon–hydrogen (C–H) bond functionalization represent one of the most step-and …

Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the
T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This …

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, gefitinib and erlotinib are
effective therapies against mutant non-small cell lung cancers (NSCLCs). Treatment is …

Ponatinib is a tyrosine kinase inhibitor (TKI) directed against BCR-ABL1 which is
successfully used in patients with BCR-ABL1 T315I+ chronic myeloid leukemia (CML) …

Given the wide spectrum of biological activities, benzothiazoles represent privileged
scaffolds in medicinal chemistry, useful in drug discovery programs to modulate biological …

Kinases have emerged as ubiquitous but highly challenging targets for drug discovery. The
human genome has 518 kinases1 and many of these play critical roles in cell growth and …

In most patients with chronic myeloid leukemia (CML) clonal cells can be kept under control
by BCR:: ABL1 tyrosine kinase inhibitors (TKI). However, overt resistance or intolerance …