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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Nuvectis Pharma announces encouraging preliminary data from the NXP800 phase 1b clinical trial in platinum-resistant ARID1a-mutated ovarian cancer. There is a 33% response rate and 100% disease control rate in patients evaluated for efficacy.
Heat shock transcription factor 1 (HSF1) is critical for tumorigenesis and progression, and is implicated in multiple solid tumors. NXP800 is a potent, clinical stage inhibitor of the HSF1 pathway. The compound activates GCN2 kinase, that phosphorylates the eIF2α and later encodes the ATF4 transcription regulator, resulting in cancer cell death. NXP800 previously gets Fast Track Designation for platinum-resistant, ARID1a-mutated ovarian cancer.
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