Quinolines are an important class of biologically active heterocyclic compounds, and their derivatives usually exhibit a variety of biological activities. They can be used as antimalarial drugs and in the preparation of other antimalarial drugs. Other important activities of quinoline derivatives include inhibitory activity against EGFR-TK and antipsychotic activity. Futhermore, quinoline scaffolds are present in various drug molecules, including the antimalarial drugs aablaquine, chloroquine, mefloquine and primaquine, and the antibacterial agents gatifloxacin, levofloxacin, and moxifloxacin.
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Epstein–Barr virus (EBV) has been associated with malignant lymphomas of B-cell, T-cell, and NK-cell origin. EBV infection of lymphoma cells leads to the development of cancers with an unmet medical need. The innovative ‘Kick and Kill’ approach targets EBV with Nanatinostat and Valganciclovir, in which Nanatinostat activates Ganciclovir by inducing the expression of EBV kinase genes. Ganciclovir then converts to cytotoxic form and results in apoptosis
Histone deacetylase (HDAC) is involved in the regulation of gene expression. HDAC inhibition induces cell cycle arrest and reactivates normal expression of tumor cells. Nanatinostat is such a potent hydroxamic acid-based class I-selective HDAC inhibitor. Nanatinostat is being studied with the antiviral agent Valganciclovir in EBV-associated malignancies. Viracta Therapeutics recently reports positive topline Nana-val results from stage 1 of the NAVAL-1 Trial from both arms of the relapsed or refractory (R/R) Epstein-Barr virus-positive (EBV+) peripheral T-cell lymphoma (PTCL) cohort.