pyrrolopyrimidine has been researched along with Lymphoma--Mantle-Cell* in 1 studies
1 other study(ies) available for pyrrolopyrimidine and Lymphoma--Mantle-Cell
| Article | Year |
|---|---|
Design and synthesis of novel substituted benzyl pyrrolopyrimidine derivatives as selective BTK inhibitors for treating mantle cell lymphoma.
Ibrutinib, a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor, was approved by the FDA for treating mantle cell lymphoma (MCL). Although ibrutinib exhibited excellent antitumor activity, it was associated with certain adverse reactions, with off-target effects against EGFR, Itk and Src family kinases. Our studies yielded a novel series of substituted benzyl pyrrolopyrimidine derivatives capable of potent inhibition of BTK. Compared with ibrutinib, compound 15c exhibited potent BTK inhibitory activity and enhanced antiproliferative activity, a 12-24-fold increase, against MCL cell lines, with IC Topics: Agammaglobulinaemia Tyrosine Kinase; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Humans; Lymphoma, Mantle-Cell; Molecular Docking Simulation; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Reactive Oxygen Species; Structure-Activity Relationship | 2021 |