Abstract Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …

Nine new fluorine-containing drugs have been approved by the US Food and Drug
Administration (FDA) in 2021, which are presented in this review article. These small …

The phospatidylinositol-3 kinase (PI3K) pathway is a crucial intracellular signaling pathway
which is mutated or amplified in a wide variety of cancers including breast, gastric, ovarian …

PURPOSE Phosphatidylinositol-3-kinase (PI3K) inhibitors have shown activity in relapsed or
refractory (R/R) indolent non-Hodgkin lymphoma (iNHL). PI3K inhibitors have been …

This review describes the recent Food and Drug Administration (FDA)-approved drugs (in
the year 2021) containing at least one halogen atom (covalently bound). The structures …

Fluorine-containing small molecules have occupied an especial position in drug discovery
research. The successful clinical use of fluorinated corticosteroids in the 1950s and …

Safety profiles of oral PI3K inhibitors have resulted in US FDA black box warnings regarding
fatal/serious toxicities. The approved intravenous PI3K inhibitor copanlisib has low …

Immunotherapy has led to a paradigm shift in the treatment of cancer. Current cancer
immunotherapies are mostly antibody-based, thus possessing advantages in regard to …

During the past 5 years, a number of highly active novel agents, including kinase inhibitors
targeting BTK or PI3Kδ, an antagonist of the antiapoptotic protein BCL-2, and new anti …

Pyrazole is a five-membered heterocycle bearing two adjacent nitrogen atoms. Both
pharmaceutical agents and natural products with pyrazole as a nucleus have exhibited a …