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Orbitrap HRMS‐Based Comprehensive Metabolite Characterization of Duvelisib in Cross‐Species Hepatocytes
Duvelisib (DVB), a selective PI3K‐δ/γ inhibitor approved for chronic lymphocytic leukemia, requires detailed metabolic characterization to support early drug development and selection of appropriate toxicology species. Because drug metabolism varies across species, an integrated system such as primary hepatocytes conta...
Novel tetrazole annulation on benzopyridodiazepine derivatives as inhibitor of tropomyosin kinase B (TrkB): rational design, synthesis, biological evaluation, SAR, and in silico studies
Four new series of tetrazole annulated benzopyridodiazepine derivatives are synthesized, especially 14h, which shows significant inhibition of TrkB in neuroblastoma cells, indicating that the tetrazole annulated benzopyridodiazepine is an interesting molecule for exploration in the management of cancer and neurological...