Fluorinated pyrimidine-5-carboxamide MERTK inhibitors with nanomolar potency and >5-fold selectivity over AXL, TYRO3, and FLT3, with leading compounds being 1a, 2c and 3b. Potential 18F-PET radioligands to image protective microglia in MS.
Cancer remains a major global health challenge and a leading cause of mortality. This ongoing burden underscores the need for continuous exploration of novel therapeutic strategies, prompting extensive review of emerging targets, mechanisms, and treatment approaches.
The 3H-pyrazolo[4,3-f]quinoline core, a privileged fusion moiety from quinoline and indazole, facilely synthesized in a one flask multi-component Doebner–Povarov reaction, is a newly described kinase hinge binder.
Indirubin, an active component of the traditional Chinese medicine Indigo Naturalis, has drawn significant attention owing to its remarkable anti-leukemia activity.
Novel FLT3/CHK1 dual agents, the representative compound 30, with favorable oral PK properties, can overcome multiple FLT3-TKD and FLT3-ITD mutations.