Benzodioxanes are a class of isomeric compounds with the molecular formula C8H8O2. The three isomers of benzodioxane are 1,2-benzodioxane, 1,3-benzodioxane and 1,4-benzodioxane. 1,4-Benzodioxane has long been a versatile template widely used to design molecules with diverse biological activities. Its use spans past decades in medicinal chemistry to today, involving many drug discovery strategies, not excluding the most advanced ones. 1,4-Benzodioxane derivatives have been described as agonists and antagonists of nicotinic, alpha-adrenergic and 5-HT receptor subtypes. 1,4-Benzodioxane derivatives have been also reported as antitumor and antibacterial agents.
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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